Those side effects, he explained, mainly come from another receptor, the mu opioid receptor.
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All drugs that exhibit efficacy at a specific receptor are known as "agonists" at that receptor.
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We do studies where we modify a receptor and mutate different amino acids in the receptor.
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Genes govern the production of each kind of receptor; the more genes, the more kinds of receptor.
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These opioids relieve pain largely by activating a specific type of opioid receptor, known as the mu receptor.
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These cannabinoids bind to one of two receptors in our brains: the CB1 receptor and the CB2 receptor.
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People get stoned when an ingredient in marijuana called THC binds to a receptor called cannabinoid receptor 1, or CB1.
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"The virus has a way of attaching to a specific receptor on lung cells called the ACE2 receptor," he said.
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But the researchers honed in on one promising receptor, the kappa opioid receptor (KOR), sussing out the structure that activates it.
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"This receptor was one of the most difficult to study given how unstable the receptor is," Stevens wrote in an email.
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Neurological problems can be caused by too much of a brain receptor called N-methyl-D-aspartate (NMDA receptor for short).
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The advantage of this strain is that it has a human receptor on its cells called an ACE2 receptor, thus its name.
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Specifically, sugar increases the concentration of a type of excitatory receptor called D1, but decreases another receptor type called D2, which is inhibitory.
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This study suggests that, in mice at least, ketamine is not working directly on the NMDA receptor, but rather on another glutamate receptor.
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The virus creates a new cell receptor -- which is, in Novartis' case, part mouse -- that targets another receptor on the cancer cells: CD19.
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What they did: The researchers looked at a different but closely related receptor (called nociceptin) to target, along with the traditional mu receptor.
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When the drug binds or sticks to one particular serotonin receptor (the serotonin 2A receptor to be exact), it changes the shape of the receptor, and that leads to a number of downstream effects, such as hallucinations and altered states of consciousness.
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THC, explains Earleywine, is a partial agonist of the CB1 receptor, which means it binds to that receptor and causes it to fire differently.
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This region of DNA encodes a brain receptor called tachykinin receptor 3, which links to the release of the hormone estrogen in the body.
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Anti-NMDA receptor encephalitis, then, happens when an otherwise healthy person's immune system makes a mistake, and starts making antibodies that affect this receptor.
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But because the drug affects estrogen receptors in the body, it only works against cancers that are estrogen-receptor-positive or progesterone-receptor positive.
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In the case of hallucinogens, signaling of the serotonin-1a receptor drives contentment, whereas signaling of the serotonin-2a receptor drives the mystical experience.
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"Once LSD gets in the receptor, a lid comes over the LSD, so it's basically trapped in the receptor and can't get out," said Roth.
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First, doctors take the patient's white blood cells, or T cells, out of the body and add a special receptor called a chimeric antigen receptor (CAR).
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Although the precise details vary from receptor to receptor, when a GPCR binds to the proper molecule, it sets off a signaling cascade within the cell.
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These effects are not precisely known, though CBD certainly has some impact on CB1's sister receptor (CB2) as well as a receptor called 5-HT1A.
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The most common forms of breast cancer, Luminal A and Luminal B, express the receptor for estrogen and are commonly known as estrogen receptor (ER-positive) tumors.
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"Our interest in nitrous oxide is that we know it blocks a certain receptor that's important in how memories are stabilised—that's called the NMDA receptor," explained Das.
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In Cahalan's case, those antibodies were directed against a receptor in her brain: the NMDA receptor, which plays a role in how brain cells communicate with each other.
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"I didn't expect that a mutation in the receptor would be so dramatic in humans," says Luis de Lecea, a biologist at Stanford who first identified the receptor in 2004.
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A team of scientists from around the globe published a study in The Cell that shows the molecular structure of your cannabinoid receptor 1, the receptor in your brain which processes THC.
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Once the team succeeded in crystalizing a CB1 receptor, they found that it had a complex "binding pocket network" which dictates how different compounds bind to the receptor and activate its effects.
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The exact cause of CHS is unknown, but is hypothesized to result from a buildup of cannabinoid compounds in the brain that leads to a "boy who cried wolf" phenomenon of the CB303 receptor: After being stimulated continuously for so long, the brain stops making the CB1 receptor, and even removes the CB1 receptor from the surface of neurons.
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Recent research has demonstrated that the signalling cascades resulting in painkilling on one hand and respiratory suppression on the other are in fact distinct, despite originating with the same receptor (the mu receptor).
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Working with embryos, He disabled the CCR5 gene, which encodes for a receptor that, along with another receptor, serves as a gateway for the HIV virus to penetrate and infect white blood cells.
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It's used in the early stages of drug development: By choosing a receptor to target, researchers could cycle through tens of thousands of compound models, looking for one that might activate the receptor.
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The Food and Drug Administration granted the designation to LEE011 in combination with letrozole for treating hormone receptor positive, human epidermal growth factor receptor 2-negative (HR+/HER2-) advanced or metastatic breast cancer.
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Receptor positive breast cancers are often responsive to hormone treatments.
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He was looking to better understand the T cell receptor.
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The tumors are all estrogen receptor negative and HER2 positive.
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Ketamine happened to be very good at blocking that receptor.
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It could only infect the ones that carried the receptor.
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A key receptor here is the NMDA receptor, which appears to have an effect on both depression and thoughts of suicide although the effect on thoughts of suicide is somewhat independent of improvements in depression.
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It's going to trigger the same response in the same receptor.
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CBD, on the other hand, doesn't affect that receptor at all.
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" Other teams wound up decoding the T-cell receptor genes. "Yeah.
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Those drugs target the CGRP molecule itself, instead of its receptor.
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"It's a pattern of receptor responses," says Aromyx founder Chris Hanson.
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"There's no 'noxious scent' receptor in the dog's brain," she added.
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So that showed the receptor we found was the right one.
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Unlike with THC, CBD's effects aren't limited to that single receptor.
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Decoy receptor 2 (DCR2), also known as TRAIL receptor 4 (TRAILR4) and tumor necrosis factor receptor superfamily member 10D (TNFRSF10D), is a human cell surface receptor of the TNF-receptor superfamily.
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Decoy receptor 1 (DCR1), also known as TRAIL receptor 3 (TRAILR3) and tumor necrosis factor receptor superfamily member 10C (TNFRSF10C), is a human cell surface receptor of the TNF-receptor superfamily.
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The IGFs are known to bind the IGF-1 receptor, the insulin receptor, the IGF-2 receptor, the insulin-related receptor and possibly other receptors. The IGF-1 receptor is the "physiological" receptor—IGF-1 binds to it at significantly higher affinity than it binds the insulin receptor. Like the insulin receptor, the IGF-1 receptor is a receptor tyrosine kinase—meaning the receptor signals by causing the addition of a phosphate molecule on particular tyrosines. The IGF-2 receptor only binds IGF-2 and acts as a "clearance receptor"—it activates no intracellular signaling pathways, functioning only as an IGF-2 sequestering agent and preventing IGF-2 signaling.
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Calcitonin receptor-like (CALCRL), also known as the calcitonin receptor-like receptor (CRLR), is a human protein; it is a receptor for calcitonin gene- related peptide.
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Death receptor 5 (DR5), also known as TRAIL receptor 2 (TRAILR2) and tumor necrosis factor receptor superfamily member 10B (TNFRSF10B), is a cell surface receptor of the TNF-receptor superfamily that binds TRAIL and mediates apoptosis.
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Death receptor 4 (DR4), also known as TRAIL receptor 1 (TRAILR1) and tumor necrosis factor receptor superfamily member 10A (TNFRSF10A), is a cell surface receptor of the TNF-receptor superfamily that binds TRAIL and mediates apoptosis.
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The JAK2 gene encodes a member of the Janus kinase family of non-receptor tyrosine kinase, JAK2. The JAK2 protein associates with the cytoplasmic tails of various cytokine and growth factor receptors that reside on the cell surface and regulate Haematopoiesis, i.e. the development and growth of blood cells. Examples of such receptors include the erythropoietin receptor, Thrombopoietin receptor, granulocyte colony-stimulating factor receptor, Granulocyte macrophage colony- stimulating factor receptor, Interleukin-3 receptor, Interleukin-5 receptor, Interleukin-6 receptor, and the receptor Thymic stromal lymphopoietin, which is a complex composed of the CRLF2 receptor combined with alpha chain of the IL-7 receptor.
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A receptor modulator, or receptor ligand, is a type of drug which binds to and modulates receptors. They are ligands and include receptor agonists and receptor antagonists, as well as receptor partial agonists, inverse agonists, and allosteric modulators.
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Examples of orphan receptors are found in the G protein-coupled receptor (GPCR) and nuclear receptor families. If an endogenous ligand is found, the orphan receptor is "adopted" or "de- orphanized". An example is the nuclear receptor Farnesoid X receptor (FXR) and the GPCR TGR5/GPCR19/G protein-coupled bile acid receptor, both of which are activated by bile acids. Adopted orphan receptors in the nuclear receptor group include FXR, liver X receptor (LXR), and peroxisome proliferator- activated receptor (PPAR).
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TRIM24 has been shown to interact with Mineralocorticoid receptor, TRIM33, Estrogen receptor alpha and Retinoid X receptor alpha.
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Like other proteins, the somatostatin receptor 2 also has variants. Somatostatin receptor 2 exists in two isoforms that are different in carboxy-terimini compositions and size. Alternative splicing of the somatostatin receptor 2 mRNA resulted in two variants, somatostatin receptor 2a (SSTR2A) and somatostatin receptor 2b (SSTR2B). In a rodent, somatostatin receptor 2a is longer compared to the shorter somatostatin receptor 2b.
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While Iloprost is an analog of PGI2 that activates PGI2's receptor, the Prostacyclin receptor, to stimulate vasodilation, it has little selectivity in that it binds to and activates all four receptors for prostaglandin E2 viz., Prostaglandin EP1 receptor, Prostaglandin EP2 receptor, Prostaglandin EP3 receptor, and Prostaglandin EP4 receptor. Activation of the EP2 and EP4 receptors cause vasodilation but activation of the EP3 receptor causes vasoconstriction.
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As a drug approaches a receptor, the receptor alters the conformation of its binding site to produce drug—receptor complex.
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In the TGF-β pathway, TGF-β dimers are recognized by a transmembrane receptor, known as type II receptor. Once the type II receptor is activated by the binding of TGF-β, it phosphorylates a type I receptor. Type I receptor is also a cell surface receptor. This receptor then phosphorylates intracellular receptor regulated SMADS (R-SMADS) such as SMAD2 or SMAD3. The phosphorylated R-SMADS then bind to SMAD4. The R-SMADs-SMAD4 association is a heteromeric complex.
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An additional opioid receptor was later identified and cloned based on homology with the cDNA. This receptor is known as the nociceptin receptor or ORL1 (opiate receptor-like 1). The opioid receptor types are nearly 70% identical, with the differences located at the N and C termini. The μ receptor is perhaps the most important.
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The C5a receptor also known as complement component 5a receptor 1 (C5AR1) or CD88 (Cluster of Differentiation 88) is a G protein-coupled receptor for C5a. It functions as a complement receptor. C5a receptor modulates inflammatory responses, obesity, development and cancers. C5a receptor structure and its residues possessing role in ligand binding or signaling.
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Type II nuclear receptors include principally subfamily 1, for example the retinoic acid receptor, retinoid X receptor and thyroid hormone receptor.
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Interleukin 28 receptor, alpha subunit is a subunit for the interleukin-28 receptor. IL28RA is its human gene. The protein encoded by this gene belongs to the class II cytokine receptor family. This protein forms a receptor complex with interleukin 10 receptor, beta (IL10RB).
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Interleukin 20 receptor, alpha subunit is a subunit for the interleukin-20 receptor. IL20RA is its human gene. The protein encoded by this gene is a receptor for interleukin 20 (IL20), a cytokine that may be involved in epidermal function. The receptor of IL20 is a heterodimeric receptor complex consisting of this protein and interleukin 20 receptor beta (IL20B).
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They bind to TGF-beta receptor type-2 (TGFBR2). Nodal binds to activin A receptor, type IIB ACVR2B. It can then either form a receptor complex with activin A receptor, type IB (ACVR1B) or with activin A receptor, type IC (ACVR1C). When the receptor- ligand binding occurs via local action, this is classified as paracrine signalling.
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The MAS1 oncogene (MAS receptor) is a G protein-coupled receptor, which binds the angiotensin-II metabolite Angiotensin (1-7). The MAS1 receptor when activated by binding angiotensin-(1-7) opposes many of the effects of angiotensin-II activated angiotensin receptor. Hence MAS1 receptor agonists have similar therapeutic effects as angiotensin-II receptor antagonists including lowering blood pressure.
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Interleukin-15 receptor is a type I cytokine receptor, binding interleukin-15. It consists of an interleukin 15 receptor, alpha subunit and shares common beta and gamma subunits with the IL-2 receptor.
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5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the HTR1B gene. The 5-HT1B receptor is a 5-HT receptor subtype.
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The interleukin-31 receptor (IL-31R) is a receptor bound and activated by interleukin-31 (IL-31). It is a heterodimer consisting of IL-31 receptor A (IL31RA) and oncostatin M receptor subunits.
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The adrenocorticotropic hormone receptor or ACTH receptor also known as the melanocortin receptor 2 or MC2 receptor is a type of melanocortin receptor (type 2) which is specific for ACTH. A G protein–coupled receptor located on the external cell plasma membrane, it is coupled to Gαs and upregulates levels of cAMP by activating adenylyl cyclase. The ACTH receptor plays a role in immune function and glucose metabolism.
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Psychedelics are 5-HT2A receptor agonists (serotonin 2A receptor agonists).
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IGF-1 binds to at least two cell surface receptors: the IGF1 Receptor (IGFR), and the insulin receptor. The IGF-1 receptor seems to be the "physiologic" receptor - it binds IGF-1 at significantly higher affinity than it binds insulin. Like the insulin receptor, the IGF-1 receptor is a receptor tyrosine kinase - meaning it signals by causing the addition of a phosphate molecule on particular tyrosines. IGF-1 activates the insulin receptor at approximately 0.1x the potency of insulin.
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Mannose and other pathogen-associated sugars, such as fucose, are recognised by the mannose receptor. Eight lectin-like domains form the extracellular part of the receptor. The ingestion mediated by the mannose receptor is distinct in molecular mechanisms from Fcγ receptor or complement receptor mediated phagocytosis.
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Figure 3. IFN dimer interacting with two IFNGR1 receptor molecules. Cellular responses to IFNγ are activated through its interaction with a heterodimeric receptor consisting of Interferon gamma receptor 1 (IFNGR1) and Interferon gamma receptor 2 (IFNGR2). IFNγ binding to the receptor activates the JAK-STAT pathway.
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Estrogen-related receptor beta (ERR-β), also known as NR3B2 (nuclear receptor subfamily 3, group B, member 2), is a nuclear receptor that in humans is encoded by the ESRRB (EStrogen Related Receptor Beta) gene .
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5-hydroxytryptamine (serotonin) 1E receptor (5-HT1E) is a highly expressed human G-protein coupled receptor that belongs to the 5-HT1 receptor family (Gi-coupled serotonin receptor). The human gene is denoted as HTR1E.
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The bile acid receptor (BAR), also known as farnesoid X receptor (FXR) or NR1H4 (nuclear receptor subfamily 1, group H, member 4) is a nuclear receptor that is encoded by the NR1H4 gene in humans.
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SSTRB receptor has approximately 300 nucleotides between carboxyl terminus and transmembrane segments fewer than the original Somatostatin receptor 2. SST2A receptor is made up of 369 amino acids and 346 amino acids make up the SST2B receptor. Somatostatin receptor 2a and somatostatin receptor 2b were found in the medulla oblongata, mesencephalon, testis, cortex, hypothalamus, hippocampus and pituitary of a rodent, using reverse transcription polymerase chain reaction (RT-PCR). Somatostatin receptor 2a is highly evident in the cortex, but the somatostatin receptor 2b is not seen as much.
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Dynorphins exert their effects primarily through the κ-opioid receptor (KOR), a G-protein-coupled receptor. Two subtypes of KORs have been identified: K1 and K2. Although KOR is the primary receptor for all dynorphins, the peptides do have some affinity for the μ-opioid receptor (MOR), δ-opioid receptor (DOR), and the N-methyl-D- aspartic acid (NMDA)-type glutamate receptor. Different dynorphins show different receptor selectivities and potencies at receptors.
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The G protein-coupled receptor kinases (GRKs) are protein kinases that phosphorylate only active GPCRs. G-protein-coupled receptor kinases (GRKs) are key modulators of G-protein-coupled receptor (GPCR) signaling. They constitute a family of seven mammalian serine-threonine protein kinases that phosphorylate agonist-bound receptor. GRKs-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling and desensitization.
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The P2X4 subunits can form homomeric or heteromeric receptors. The P2X4 receptor has a typical P2X receptor structure. The zebrafish P2X4 receptor was the first purinergic receptor to be crystallized and have its three- dimensional structure solved, forming the model for the P2X receptor family. The P2X4 receptor is a ligand-gated cation channel that opens in response to ATP binding.
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Interleukin 1 receptor, type I (IL1R1) also known as CD121a (Cluster of Differentiation 121a), is an interleukin receptor. IL1R1 also denotes its human gene. The protein encoded by this gene is a cytokine receptor that belongs to the interleukin-1 receptor family. This protein is a receptor for interleukin 1 alpha (IL1A), interleukin 1 beta (IL1B), and interleukin 1 receptor antagonist (IL1RA).
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Estrogen receptor alpha (ERα), also known as NR3A1 (nuclear receptor subfamily 3, group A, member 1), is one of two main types of estrogen receptor, a nuclear receptor that is activated by the sex hormone estrogen. In humans, ERα is encoded by the gene ESR1 (EStrogen Receptor 1).
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Tropomyosin receptor kinase B (TrkB), also known as tyrosine receptor kinase B, or BDNF/NT-3 growth factors receptor or neurotrophic tyrosine kinase, receptor, type 2 is a protein that in humans is encoded by the NTRK2 gene. TrkB is a receptor for brain-derived neurotrophic factor (BDNF).
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During withdrawal from full or partial agonists, changes occur in benzodiazepine receptor with upregulation of some receptor subtypes and downregulation of other receptor subtypes.
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The receptor for CXCL17 is likely to be a G protein-coupled receptor (GPCR). The GPCR GPR35 was thought to be a receptor of CXCL17. Subsequent research has suggested that GPR35 is not a receptor for CXCL17.
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Oxmetidine (code name SKF 92994) is an H2 histamine receptor receptor antagonist.
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An atrial natriuretic peptide receptor is a receptor for atrial natriuretic peptide.
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LINGO-1 is a co-receptor that interacts with the ligand-binding Nogo-66 receptor (NogoR) in the Nogo receptor signaling complex. The Nogo receptor complex is formed when Nogo-66 binds to its receptor. LINGO-1 is an homotetramer which forms a ternary complex with RTN4R/NGFR and RTN4R/TNFRSF19.
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The ciliary neurotrophic factor receptor, also known as CNTFR, binds the ciliary neurotrophic factor. This receptor and its cognate ligand support the survival of neurons. This receptor is most closely related to the interleukin-6 receptor. This receptor possesses an unusual attachment to the cell membrane through a glycophosphatidylinositol linkage.
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Adenosine A2A receptor has been shown to interact with Dopamine receptor D2. As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors.
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A second type of ionotropic GABA receptor, insensitive to typical allosteric modulators of GABAA receptor channels such as benzodiazepines and barbiturates, was designated GABAС receptor. Native responses of the GABAC receptor type occur in retinal bipolar or horizontal cells across vertebrate species. GABAС receptors are exclusively composed of ρ (rho) subunits that are related to GABAA receptor subunits. Although the term "GABAС receptor" is frequently used, GABAС may be viewed as a variant within the GABAA receptor family.
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This gene encodes a bitter taste receptor; bitter taste receptors are members of the G protein-coupled receptor superfamily and are specifically expressed by taste receptor cells of the tongue and palate epithelia. Each of these apparently intronless taste receptor genes encodes a 7-transmembrane receptor protein, functioning as a bitter taste receptor. This gene is clustered with another 3 candidate taste receptor genes on chromosome 7 and is genetically linked to loci that influence bitter perception.
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The protein encoded by this gene is a glycosylphosphatidylinositol(GPI)-linked cell surface receptor and a member of the GDNF receptor family. It forms a signaling receptor complex with RET tyrosine kinase receptor and binds the ligand, artemin.
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The role of the other BDNF receptor, p75, is less clear. While the TrkB receptor interacts with BDNF in a ligand-specific manner, all neurotrophins can interact with the p75 receptor. When the p75 receptor is activated, it leads to activation of NFkB receptor. Thus, neurotrophic signaling may trigger apoptosis rather than survival pathways in cells expressing the p75 receptor in the absence of Trk receptors.
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Mannose receptor provide reception of extracellular ligands. To the family of mannose receptors belong: mannose receptor, M-phospholipase A2 receptor (PLA2R), Dec-205, Endo180/uPARAP. They share and extracellular domain, which contains N-terminal domain rich in cystein, F2 fibronectin type II domain and several C-lectin domains. From this mannose family, collagen is specifically bound by mannose receptor, M-phospholipase A2 receptor and Endo180 receptor.
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This receptor was initially named the formyl peptide receptor (i.e. FPR). However, a series of subsequent studies cloned two genes that encoded receptor-like proteins with amino acid sequences very similar to that of FPR. The three receptors had been given various names but are now termed formyl peptide receptor 1 (i.e. FPR1) for the first defined receptor, FPR2, and Formyl peptide receptor 3 (i.e. FPR3).
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Interleukin-1 receptor-like 2 is a protein that in humans is encoded by the IL1RL2 gene. The protein encoded by this gene is a member of the interleukin 1 receptor family. An experiment with transient gene expression demonstrated that this receptor was incapable of binding to interleukin 1 alpha and interleukin 1 beta with high affinity. This gene and four other interleukin 1 receptor family genes, including interleukin 1 receptor, type I (IL1R1), interleukin 1 receptor, type II (IL1R2), interleukin 1 receptor-like 1 (IL1RL1), and interleukin 18 receptor 1 (IL18R1), form a cytokine receptor gene cluster in a region mapped to chromosome 2q12.
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H1-antihistamines refer to compounds that inhibit the activity of the H1 receptor. Since the H1 receptor exhibits constitutive activity, H1-antihistamines can be either neutral receptor antagonists or inverse agonists. Normally, histamine binds to the H1 receptor and heightens the receptor's activity; the receptor antagonists work by binding to the receptor and blocking the activation of the receptor by histamine; by comparison, the inverse agonists bind to the receptor and both block the binding of histamine, and reduce its constitutive activity, an effect which is opposite to histamine's. Most antihistamines are inverse agonists at the H1 receptor, but it was previously thought that they were antagonists.
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3-MeO-PCE has Ki values of 61 nM for the NMDA receptor, 743 nM for the dopamine transporter, 2097 nM for the histamine H2 receptor, 964 nM for the alpha-2A adrenergic receptor, 115 nM for the serotonin transporter, 4519 nM for the σ1 receptor, and 525 nM for the σ2 receptor.
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Lymphotoxin beta receptor (LTBR), also known as tumor necrosis factor receptor superfamily member 3 (TNFRSF3), is a cell surface receptor for lymphotoxin involved in apoptosis and cytokine release. It is a member of the tumor necrosis factor receptor superfamily.
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The P2X7 receptor also serves as a pattern recognition receptor for extracellular ATP-mediated apoptotic cell death, regulation of receptor trafficking, mast cell degranulation, and inflammation.
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Herpesvirus entry mediator (HVEM), also known as tumor necrosis factor receptor superfamily member 14 (TNFRSF14), is a human cell surface receptor of the TNF-receptor superfamily.
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Efaroxan is an α2-adrenergic receptor antagonist and antagonist of the imidazoline receptor.
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The receptor mediates activation of the RET tyrosine kinase receptor. This encoded protein acts preferentially as a receptor for NTN compared to its other family member, GDNF family receptor alpha 1. This gene is a candidate gene for RET-associated diseases.
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The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic receptor family. The human gene encoding this receptor has the symbol ADRA2B. ADRA2B orthologs have been identified in several mammals.
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20-HETE activates the mouse and human transient receptor potential cation channel subfamily V member 1 (TRPV1, also known as the capsaicin receptor and the vanilloid receptor 1), and through this receptor, cultured dorsal root ganglion cells taken from mice.
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G protein-coupled receptor kinases phosphorylate activated G protein-coupled receptors, which promotes the binding of an arrestin protein to the receptor. Arrestin binding to phosphorylated, active receptor prevents receptor stimulation of heterotrimeric G protein transducer proteins, blocking their cellular signaling and resulting in receptor desensitization. Arrestin binding also directs receptors to specific cellular internalization pathways, removing the receptors from the cell surface and also preventing additional activation. Arrestin binding to phosphorylated, active receptor also enables receptor signaling through arrestin partner proteins.
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G protein-coupled receptor kinases phosphorylate activated G protein-coupled receptors, which promotes the binding of an arrestin protein to the receptor. Arrestin binding to phosphorylated, active receptor prevents receptor stimulation of heterotrimeric G protein transducer proteins, blocking their cellular signaling and resulting in receptor desensitization. Arrestin binding also directs receptors to specific cellular internalization pathways, removing the receptors from the cell surface and also preventing additional activation. Arrestin binding to phosphorylated, active receptor also enables receptor signaling through arrestin partner proteins.
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Oncostatin-M specific receptor subunit beta also known as the Oncostatin M receptor (OSMR) , is one of the receptor proteins for oncostatin M, that in humans is encoded by the OSMR gene. OSMR is a member of the type I cytokine receptor family. This protein heterodimerizes with interleukin 6 signal transducer to form the type II oncostatin M receptor and with interleukin 31 receptor A to form the interleukin 31 receptor, and thus transduces oncostatin M and interleukin 31 induced signaling events.
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The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor. 5-HT is short for 5-hydroxy- tryptamine, which is serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex.
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G protein-coupled receptor kinases phosphorylate activated G protein-coupled receptors, which promotes the binding of an arrestin protein to the receptor. Arrestin binding to phosphorylated, active receptor prevents receptor stimulation of heterotrimeric G protein transducer proteins, blocking their cellular signaling and resulting in receptor desensitization. Arrestin binding also directs receptors to specific cellular internalization pathways, removing the receptors from the cell surface and also preventing additional activation. Arrestin binding to phosphorylated, active receptor also enables receptor signaling through arrestin partner proteins.
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G protein-coupled receptor kinases phosphorylate activated G protein-coupled receptors, which promotes the binding of an arrestin protein to the receptor. Arrestin binding to phosphorylated, active receptor prevents receptor stimulation of heterotrimeric G protein transducer proteins, blocking their cellular signaling and resulting in receptor desensitization. Arrestin binding also directs receptors to specific cellular internalization pathways, removing the receptors from the cell surface and also preventing additional activation. Arrestin binding to phosphorylated, active receptor also enables receptor signaling through arrestin partner proteins.
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The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human adenosine A2b receptor gene which encodes it.
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Retinoic acid receptor gamma (RAR-γ), also known as NR1B3 (nuclear receptor subfamily 1, group B, member 3) is a nuclear receptor encoded by the RARG gene.
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Adenosine A2A receptor antagonists are a class of drugs that blocks adenosine at the adenosine A2A receptor. Notable adenosine A2A receptor antagonists include caffeine, theophylline and istradefylline.
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The thromboxane receptor (TP) also known as the prostanoid TP receptor is a protein that in humans is encoded by the TBXA2R gene, The thromboxane receptor is one among the five classes of prostanoid receptors and was the first eicosanoid receptor cloned. The TP receptor derives its name from its preferred endogenous ligand thromboxane A2.
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This gene encodes a member of a family of candidate taste receptors that are members of the G protein-coupled receptor superfamily and that are specifically expressed by taste receptor cells of the tongue and palate epithelia. This intronless taste receptor gene encodes a 7-transmembrane receptor protein, functioning as a bitter taste receptor.
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BAFF receptor (B-cell activating factor receptor, BAFF-R), also known as tumor necrosis factor receptor superfamily member 13C (TNFRSF13C) and BLyS receptor 3 (BR3), is a membrane protein of the TNF receptor superfamily which recognizes BAFF, an essential factor for B cell maturation and survival. In humans it is encoded by the TNFRSF13C gene.
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The interleukin-5 receptor is a type I cytokine receptor. It is a heterodimer of the interleukin 5 receptor alpha subunit and CSF2RB. The IL-5 receptor (IL-5R) belongs to the type I cytokine receptor family and is a heterodimer composed of two polypeptide chains, one α subunit, which binds IL-5 and confers upon the receptor cytokine specificity, and one β subunit, which contains the signal transduction domains.
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Previous studies have shown that GPCRs can form heterodimers, or functional receptor pairs with other types of G-protein coupled receptors (GPCRs). Various studies suggest that GHS-R1a specifically forms dimers with the following hormone and neurotransmitter receptors: somatostatin receptor 5, dopamine receptor type 2 (DRD2), melanocortin-3 receptor (MC3R), and serotonin receptor type 2C (5-HT2c receptor). See "Function" section below for details on the purported functions of these heterodimers.
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Somatostatin receptor 2b is not shown expressed without somatostatin receptor 2a in the brain.
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ACP1 has been shown to interact with EPH receptor A2 and EPH receptor B1.
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Liver X receptor alpha (LXR-alpha) is a nuclear receptor protein that in humans is encoded by the NR1H3 gene (nuclear receptor subfamily 1, group H, member 3).
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Nicotine acts as a receptor agonist at most nicotinic acetylcholine receptors (nAChRs), except at two nicotinic receptor subunits (nAChRα9 and nAChRα10) where it acts as a receptor antagonist.
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On cells, Interleukin-6 binds to an Interleukin-6 receptor, which, however, is not signaling. The complex of Interleukin-6 and the Interleukin-6 receptor binds to a second receptor protein, gp130, which thereupon dimerizes and initiates intracellular. The gp130 receptor is present on all cells of the human body, whereas the Interleukin-6 receptor is only expressed by some cells such as hepatocytes and some leukocytes. Since Interleukin-6 exhibits only measurable affinity to the Interleukin-6 receptor but not to gp130, only cells which express the Interleukin-6 receptor can respond to Interleukin-6. It was found that the Interleukin-6 receptor can be cleaved from the cell membrane by the protease ADAM17 generating a soluble receptor. Interestingly, the soluble Interleukin-6 receptor can still bind Interleukin-6 and the complex of Interleukin-6 and Interleukin-6 receptor can bind to gp130 even on cells, which do not express the membrane-bound Interleukin-6 receptor.
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In enzymology, a beta-adrenergic-receptor kinase () is an enzyme that catalyzes the chemical reaction: :ATP + [beta-adrenergic receptor] \rightleftharpoons ADP + phospho-[beta-adrenergic receptor] Thus, the two substrates of this enzyme are ATP and beta-adrenergic receptor, whereas its two products are ADP and phospho-beta-adrenergic receptor. This enzyme belongs to the family of transferases, specifically those transferring a phosphate group to the sidechain oxygen atom of serine or threonine residues in proteins (protein-serine/threonine kinases). The systematic name of this enzyme class is ATP:[beta-adrenergic receptor] phosphotransferase. Other names in common use include ATP:beta-adrenergic-receptor phosphotransferase, [beta-adrenergic- receptor] kinase, beta-adrenergic receptor-specific kinase, beta-AR kinase, beta-ARK, beta-ARK 1, beta-ARK 2, beta-receptor kinase, GRK2, GRK3, beta- adrenergic-receptor kinase (phosphorylating), beta2ARK, betaARK1, beta- adrenoceptor kinase, beta-adrenoceptor kinase 1, beta-adrenoceptor kinase 2, ADRBK1, BARK1, adrenergic receptor kinase, and STK15.
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Tyrosine-protein kinase transmembrane receptor ROR1, also known as neurotrophic tyrosine kinase, receptor-related 1 (NTRKR1), is an enzyme that in humans is encoded by the ROR1 gene. ROR1 is a member of the receptor tyrosine kinase-like orphan receptor (ROR) family.
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Testicular receptor 4 also known as NR2C2 (nuclear receptor subfamily 2, group C, member 2) is a protein that in humans is encoded by the NR2C2 gene. The testicular receptor 4 is a member of the nuclear receptor family of transcription factors.
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Small molecule antagonists of CCR5 bind to a hydrophobic pocket formed by the transmembrane helices of the CCR5 receptor. They are thought to interact with the receptor in an allosteric manner locking the receptor in a conformation that prohibits its co-receptor function.
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Peroxisome proliferator-activated receptor gamma (PPAR-γ or PPARG), also known as the glitazone receptor, or NR1C3 (nuclear receptor subfamily 1, group C, member 3) is a type II nuclear receptor (protein regulating genes) that in humans is encoded by the PPARG gene.
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A hormone-receptor-positive (HR+) tumor is a tumor which consists of cells that express receptors for certain hormones. The term most commonly refers to estrogen receptor positive tumors (i.e. tumors that contain estrogen receptor positive cells), but can also include progesterone receptor positive tumors. Estrogen-receptor-positive tumors depend on the presence of estrogen for ongoing proliferation.
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Lanthanide probes displays unique fluorescence properties, including long lifetime of fluorescence, large Stokes shift and narrow emission peak. These properties is highly advantageous to develop analytical probes for receptor-ligand interactions. Many lanthanide-based fluorescence studies have been developed for GPCRs, including CXCR1, insulin-like family peptide receptor 2, protease-activated receptor 2, β2-adrenergic receptor and C3a receptor.
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The tachykinin receptor 1 (TACR1) also known as neurokinin 1 receptor (NK1R) or substance P receptor (SPR) is a G protein coupled receptor found in the central nervous system and peripheral nervous system. The endogenous ligand for this receptor is Substance P, although it has some affinity for other tachykinins. The protein is the product of the TACR1 gene.
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SAS-1121 is a norbenzomorphan-piperazine that is highly selective for the sigma-2 receptor over the sigma-1 receptor. SAS-1121 is 280-fold selective for the sigma 2 receptor (Ki = 23.8 nM) over the sigma 1 receptor (Ki = 6659.6 nM) and served as a tool compound to help identify the sigma 2 receptor as transmembrane 97 (TMEM97).
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Antiadrenergic agents inhibit the signals of epinephrine and norepinephrine. They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers"), inhibiting the downstream cellular signaling pathways of adrenergic receptors. However, there are exceptions: clonidine is an adrenergic agonist at the α2 receptor; since this receptor is located presynaptically, agonism at this receptor inhibits the presynaptic release of adrenaline and noradrenaline, preventing postsynaptic adrenergic receptor activation and downstream signaling. Another way to inhibit adrenergic receptor signaling is by blocking the synthesis of catecholamines.
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G protein-coupled receptor 32, also known as GPR32 or the RvD1 receptor, is a human Receptor (biochemistry) belonging to the rhodopsin-like subfamily of G protein-coupled receptors.
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The interleukin-28 receptor is a complex made up of two protein chains; the interleukin-28 receptor alpha chain and the beta chain from another interleukin receptor (IL-10).
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Interleukin 8 receptor, beta is a chemokine receptor. IL8RB is also known as CXCR2, and CXCR2 is now the IUPHAR Committee on Receptor Nomenclature and Drug classification-recommended name.
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Anti-Müllerian hormone receptor is a receptor for anti-Müllerian hormone. Anti-Mullerian hormone receptor type 2 is a protein that in humans is encoded by the AMHR2 gene.
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Pearson Education, Limited, 2009. p. 12.3 The bulboid corpuscle, is a cutaneous receptor a cold-sensitive receptor, that detects cold temperatures. The other type is a warmth-sensitive receptor.
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Galanin receptor 1 (GAL1) is a G-protein coupled receptor encoded by the GALR1 gene.
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Endothelin receptor type A, also known as ETA, is a human G protein-coupled receptor.
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Galanin receptor 3 (GAL3) is a G-protein coupled receptor encoded by the GALR3 gene.
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Galanin receptor 2, (GAL2) is a G-protein coupled receptor encoded by the GALR2 gene.
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S-14,506 is a phenylpiperazine, a 5-HT1A receptor agonist, and a dopamine receptor antagonist.
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CCR4 is receptor typically expressed in lesional skin only. CCR4 is a receptor for TARC.
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The interleukin 4 receptor is a type I cytokine receptor. IL4R is its human gene.
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Indeed, the main receptor of these hormone signals - the ecdysone receptor - is an intracellular protein.
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The AMPA receptor bound to a glutamate antagonist showing the amino terminal, ligand binding, and transmembrane domain, PDB 3KG2 The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor) is an ionotropic transmembrane receptor for glutamate that mediates fast synaptic transmission in the central nervous system (CNS). It has been traditionally classified as a non-NMDA-type receptor, along with the kainate receptor. Its name is derived from its ability to be activated by the artificial glutamate analog AMPA. The receptor was first named the "quisqualate receptor" by Watkins and colleagues after a naturally occurring agonist quisqualate and was only later given the label "AMPA receptor" after the selective agonist developed by Tage Honore and colleagues at the Royal Danish School of Pharmacy in Copenhagen.
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Estrogen-related receptor alpha (ERRα), also known as NR3B1 (nuclear receptor subfamily 3, group B, member 1), is a nuclear receptor that in humans is encoded by the ESRRA (Estrogen Related Receptor Alpha) gene. ERRα was originally cloned by DNA sequence homology to the estrogen receptor alpha (ERα, NR3A1), but subsequent ligand binding and reporter-gene transfection experiments demonstrated that estrogens did not regulate ERRα. Currently, ERRα is considered an orphan nuclear receptor.
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The luteinizing hormone/choriogonadotropin receptor (LHCGR), also lutropin/choriogonadotropin receptor (LCGR) or luteinizing hormone receptor (LHR) is a transmembrane receptor found predominantly in the ovary and testis, but also many extragonadal organs such as the uterus and breasts. The receptor interacts with both luteinizing hormone (LH) and chorionic gonadotropins (such as hCG in humans) and represents a G protein-coupled receptor (GPCR). Its activation is necessary for the hormonal functioning during reproduction.
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Hundreds of modified compounds were synthesized in an effort to develop a model of the receptor. The first breakthrough was Nα-guanylhistamine, a partial H2 receptor antagonist. From this lead, the receptor model was further refined and eventually led to the development of burimamide, the first H2 receptor antagonist. Burimamide, a specific competitive antagonist at the H2 receptor, 100 times more potent than Nα-guanylhistamine, proved the existence of the H2 receptor.
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The thyrotropin receptor (TSH receptor) is the antigen for TSH receptor antibodies (TRAbs). It is a seven transmembrane G protein-coupled receptor that is involved in thyroid hormone signalling. TRAbs are grouped depending on their effects on receptor signalling; activating antibodies (associated with hyperthyroidism), blocking antibodies (associated with thyroiditis) and neutral antibodies (no effect on receptor). Activating and blocking antibodies mostly bind to conformational epitopes, whereas neutral antibodies bind to linear epitopes.
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The low-affinity nerve growth factor receptor (nerve growth factor receptor (TNFR superfamily, member 16), also called the LNGFR or p75 neurotrophin receptor) is one of the two receptor types for the neurotrophins, a family of protein growth factors that stimulate neuronal cells to survive and differentiate. LNGFR is a member of the tumor necrosis factor receptor (TNF receptor)superfamily – indeed, LNGFR was the first member of this large family of receptors to be characterized.
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5-HT5B receptor is a 5-HT receptor protein and the gene which encodes it. The protein is found in rodents, but not in humans, because stop codons in the gene's coding sequence prevent the gene from expressing a functional protein. It is believed that the function of the 5-HT5B receptor has been replaced in humans by some other subclass of 5-HT receptor. 5-HT5B receptor is a G protein-coupled receptor.
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The 5HT6 receptor is a subtype of 5HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5HT). It is a G protein- coupled receptor (GPCR) that is coupled to Gs and mediates excitatory neurotransmission. HTR6 denotes the human gene encoding for the receptor.
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The receptor was identified among cDNAs based on its similarity in amino-acid sequence to the cannabinoid receptor type 1 (CB1) receptor, discovered in 1990. The discovery of this receptor helped provide a molecular explanation for the established effects of cannabinoids on the immune system.
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The muscle-type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination (α1)2β1δε (adult receptor) or (α1)2β1δγ (fetal receptor). It is located in the neuromuscular junction, where activation yields EPSP, mainly by increased Na+ and K+ conductance.
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Estrogen receptor beta (ERβ), also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2), is one of two main types of estrogen receptor, a nuclear receptor which is activated by the sex hormone estrogen. In humans, ERβ is encoded by the ESR2 gene.
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Death receptor 3 (DR3), also known as tumor necrosis factor receptor superfamily member 25 (TNFRSF25), is a cell surface receptor of the tumor necrosis factor receptor superfamily which mediates apoptotic signalling and differentiation. Its only known TNFSF ligand is TNF-like protein 1A (TL1A).
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Tumor necrosis factor receptor 2 (TNFR2), also known as tumor necrosis factor receptor superfamily member 1B (TNFRSF1B) and CD120b, is a membrane receptor that binds tumor necrosis factor-alpha (TNFα).
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Pyroglutamylated RFamide peptide receptor also known as orexigenic neuropeptide QRFP receptor or G-protein coupled receptor 103 (GPR103) is a protein that in humans is encoded by the QRFPR gene.
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CD120 (Cluster of Differentiation 120) can refer to two members of the tumor necrosis factor receptor superfamily: tumor necrosis factor receptor 1 (TNFR1) and tumor necrosis factor receptor 2 (TNFR2).
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Natriuretic peptide receptor A/guanylate cyclase A (atrionatriuretic peptide receptor A), also known as NPR1, is an atrial natriuretic peptide receptor. In humans it is encoded by the NPR1 gene.
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Natriuretic peptide receptor B/guanylate cyclase B (atrionatriuretic peptide receptor B), also known as NPR2, is an atrial natriuretic peptide receptor. In humans it is encoded by the NPR2 gene.
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Natriuretic peptide receptor C/guanylate cyclase C (atrionatriuretic peptide receptor C), also known as NPR3, is an atrial natriuretic peptide receptor. In humans it is encoded by the NPR3 gene.
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The protein encoded by this gene belongs to the G protein-coupled receptor family that activate a phosphatidylinositol-calcium second messenger system. Binding and pharmacological studies demonstrate that this receptor binds neurotensin as well as several other ligands already described for neurotensin NT1 receptor. However, unlike NT1 receptor, this gene recognizes, with high affinity, levocabastine, a histamine H1 receptor antagonist previously shown to compete with neurotensin for low-affinity binding sites in brain. These activities suggest that this receptor may be of physiological importance and that a natural agonist for the receptor may exist.
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Arylcyclohexylamines varyingly possess NMDA receptor antagonistic, dopamine reuptake inhibitory, and μ-opioid receptor agonistic properties. Additionally, σ receptor agonistic, nACh receptor antagonistic, and D2 receptor agonistic actions have been reported for some of these agents. Antagonism of the NMDA receptor confers anesthetic, anticonvulsant, neuroprotective, and dissociative effects; blockade of the dopamine transporter mediates stimulant and euphoriant effects as well as psychosis in high amounts; and activation of the μ-opioid receptor causes analgesic and euphoriant effects. Stimulation of the σ and D2 receptors may also contribute to hallucinogenic and psychotomimetic effects.
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The transient receptor potential cation channel subfamily V member 1 (TrpV1), also known as the capsaicin receptor and the vanilloid receptor 1, is a protein that, in humans, is encoded by the TRPV1 gene. It was the first isolated member of the transient receptor potential vanilloid receptor proteins that in turn are a sub-family of the transient receptor potential protein group. This protein is a member of the TRPV group of transient receptor potential family of ion channels. The function of TRPV1 is detection and regulation of body temperature.
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Nuclear receptor coregulatorsThis article is based on the transcript of an animated course on the Nuclear Receptor Signaling Atlas (NURSA) website entitled "Nuclear receptor signaling: concepts and models". Permission to re- use this material was obtained from the original copyright holder, the Nuclear Receptor Signaling Atlas, on August 25th 2008. are a class of transcription coregulators that have been shown to be involved in any aspect of signaling by any member of the nuclear receptor superfamily. A comprehensive database of nuclear receptor coregulators can be found at the Nuclear Receptor Signaling Atlas website.
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Regulation of the calcitonin gene- related peptide (CGRP) gene is in part controlled by the expression of the mitogen-activated protein kinases (MAPK) signaling pathway, cytokines such as TNFα and iNOS. 5HT1 receptor agonists, such as sumatriptan, increase intracellular calcium, which cause decreases in CGRP promoter activity. CGRP receptor is found in myelinated A-fibers axon which is required for ligand specificity and function of the receptor. The CGRP receptor has three subunits: receptor activity-modifying protein 1 (RAMP1), calcitonin-like receptor (CLR) and receptor component protein (RCP).
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Sunitinib is an oral tyrosine kinase inhibitor that acts upon vascular endothelial growth factor receptor (VEGFR), platelet- derived growth factor receptor (PDGFR), stem cell factor receptor, and colony- stimulating factor-1 receptor (Burstein et al. 2008) Gefitinib and erlotinib inhibit the tyrosine kinase domain of epidermal growth factor receptor (EGFR), and can be used to treat lung and pancreatic cancer where there is often over- expression of this cell-surface receptor tyrosine kinase. Kinase inhibitors can also be mediated. Paracrine signalling mediates the response to epidermal growth factor receptor kinase inhibitors.
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The TrkB receptor is part of the large family of receptor tyrosine kinases. A "tyrosine kinase" is an enzyme which is capable of adding a phosphate group to certain tyrosines on target proteins, or "substrates". A receptor tyrosine kinase is a "tyrosine kinase" which is located at the cellular membrane, and is activated by binding of a ligand to the receptor's extracellular domain. Other examples of tyrosine kinase receptors include the insulin receptor, the IGF1 receptor, the MuSK protein receptor, the Vascular Endothelial Growth Factor (or VEGF) receptor, etc.
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G protein-coupled receptor kinase 4 (GRK4) is an enzyme that in humans is encoded by the GRK4 gene. This gene encodes a member of the G protein-coupled receptor kinase subfamily of the Ser/Thr protein kinase family, and is most highly similar to GRK5 and GRK6. G protein-coupled receptor kinases phosphorylate activated G protein-coupled receptors, which promotes the binding of an arrestin protein to the receptor. Arrestin binding to phosphorylated, active receptor prevents receptor stimulation of heterotrimeric G protein transducer proteins, blocking their cellular signaling and resulting in receptor desensitization.
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RBM39 has been shown to interact with Estrogen receptor alpha, Estrogen receptor beta and C-jun.
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Liver X receptor beta has been shown to interact with NCOA6 and Retinoid X receptor alpha.
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BMY-7,378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist.
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SOCS2 has been shown to interact with insulin-like growth factor 1 receptor and erythropoietin receptor.
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BRD8 has been shown to interact with Thyroid hormone receptor beta and Retinoid X receptor alpha.
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The D1–D2 dopamine receptor heteromer is a receptor heteromer consisting of D1 and D2 protomers.
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Histaminergic means "working on the histamine system", and histaminic means "related to histamine". A histaminergic agent (or drug) is a chemical which functions to directly modulate the histamine system in the body or brain. Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines). Subdivisions of histamine antagonists include H1 receptor antagonists, H2 receptor antagonists, and H3 receptor antagonists.
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The leptin hormone regulates adipose-tissue mass through hypothalamus effects on hunger and energy use. It acts through the leptin receptor (LEP-R), a single- transmembrane-domain receptor of the cytokine receptor family. In hypothalamic neurons, adequate leptin receptor function and subsequent regulation of energy metabolism and body weight depends on interactions of the receptor with gangliosides in the cell membrane.
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Interleukin 10 (IL-10), also known as human cytokine synthesis inhibitory factor (CSIF), is an anti-inflammatory cytokine. In humans, interleukin 10 is encoded by the IL10 gene. IL-10 signals through a receptor complex consisting of two IL-10 receptor-1 and two IL-10 receptor-2 proteins. Consequently, the functional receptor consists of four IL-10 receptor molecules.
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A receptor may contain one or more binding sites for different ligands. Binding to the active site on the receptor regulates receptor activation directly. The activity of receptors can also be regulated by the binding of a ligand to other sites on the receptor, as in allosteric binding sites. Antagonists mediate their effects through receptor interactions by preventing agonist-induced responses.
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Retinoic acid receptor beta (RAR-beta), also known as NR1B2 (nuclear receptor subfamily 1, group B, member 2) is a nuclear receptor that in humans is encoded by the RARB gene.
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Discovered in 2000, NADA preferentially binds to the CB1 receptor. Like anandamide, NADA is also an agonist for the vanilloid receptor subtype 1 (TRPV1), a member of the vanilloid receptor family.
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Retinoid X receptor gamma (RXR-gamma), also known as NR2B3 (nuclear receptor subfamily 2, group B, member 3) is a nuclear receptor that in humans is encoded by the RXRG gene.
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The interleukin 11 receptor is a type I cytokine receptor, binding interleukin 11. It is a heterodimer composed of an interleukin 11 receptor alpha subunit and an incompletely characterized beta subunit.
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Excitatory amino acid receptor ligands are ligands of excitatory amino acid receptors (EAARs), also known as glutamate receptors. They include excitatory amino acid receptor agonists and excitatory amino acid receptor antagonists.
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The bradykinin receptor family is a group of G-protein coupled receptors whose principal ligand is the protein bradykinin. There are two Bradykinin receptors: the B1 receptor and the B2 receptor.
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It potentiates glycine receptor activity, which decreases motor function. It inhibits receptor activity in the NMDA glutamate receptor subtypes. Isoflurane inhibits conduction in activated potassium channels. Isoflurane also affects intracellular molecules.
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Tumor necrosis factor receptor 1 (TNFR1), also known as tumor necrosis factor receptor superfamily member 1A (TNFRSF1A) and CD120a, is a ubiquitous membrane receptor that binds tumor necrosis factor-alpha (TNFα).
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Retinoid X receptor alpha (RXR-alpha), also known as NR2B1 (nuclear receptor subfamily 2, group B, member 1) is a nuclear receptor that in humans is encoded by the RXRA gene.
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Retinoic acid receptor alpha (RAR-α), also known as NR1B1 (nuclear receptor subfamily 1, group B, member 1) is a nuclear receptor that in humans is encoded by the RARA gene.
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Chemical structures of selective D1 receptor agonists. Several D1 receptor agonists are used clinically. These include apomorphine, pergolide, rotigotine, and terguride. All of these drugs are preferentially D2-like receptor agonists.
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GABA receptor types and their clinical functions. Notice that α2 receptor type refers to the GABRA2, an anxiolyte. GABAA receptor animation demonstrates the various subunit types that make up the GABA receptor. All the variants of GABA (A) receptors have different functions within the mammalian brain.
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Molecular model of the α7 nicotinic receptor. The alpha-7 nicotinic receptor, also known as the α7 receptor, is a type of nicotinic acetylcholine receptor implicated in long term memory, consisting entirely of α7 subunits.Pharmacology, (Rang, Dale, Ritter & Moore, , 5th ed., Churchill Livingstone 2003) p. 138.
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A subclass of ionotropic GABA receptors, insensitive to typical allosteric modulators of GABAA receptor channels such as benzodiazepines and barbiturates, was designated GABAС receptor. Native responses of the GABAC receptor type occur in retinal bipolar or horizontal cells across vertebrate species. GABAС receptors are exclusively composed of ρ (rho) subunits that are related to GABAA receptor subunits. Although the term "GABAС receptor" is frequently used, GABAС may be viewed as a variant within the GABAA receptor family.
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Estrogen-related receptor gamma (ERR-gamma), also known as NR3B3 (nuclear receptor subfamily 3, group B, member 3), is a nuclear receptor that in humans is encoded by the ESRRG (EStrogen Related Receptor Gamma) gene. It behaves as a constitutive activator of transcription. This protein is a member of nuclear hormone receptor family of steroid hormone receptors. No physiological activating ligand is known for this orphan receptor, but 4-hydroxytamoxifen and diethylstilbestrol act as inverse agonists and deactivate ESRRG.
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TGF Beta ligand binds to receptor The TGF beta superfamily of ligands include: Bone morphogenetic proteins (BMPs), Growth and differentiation factors (GDFs), Anti-müllerian hormone (AMH), Activin, Nodal and TGFβ's. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. Each class of ligand binds to a specific type II receptor.
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This may include VAP anti-idiotypic antibodies, natural ligands of the receptor and anti-receptor antibodies. # Using agents which mimic the cellular receptor and bind to the VAP. This includes anti-VAP antibodies, receptor anti-idiotypic antibodies, extraneous receptor and synthetic receptor mimics. This strategy of designing drugs can be very expensive, and since the process of generating anti-idiotypic antibodies is partly trial and error, it can be a relatively slow process until an adequate molecule is produced.
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Figure 1 The four main regions of the androgen receptor The AR belongs to the steroid receptor subfamily of the nuclear receptor superfamily. Its function is regulated by the binding of androgens, which initiates sequential conformation changes of the receptor that affects receptor-protein and receptor-DNA interactions. Endogenous androgens are mainly testosterone and DHT. AR is expressed in cells of a wide range of tissues, throughout the entire body, beyond primary and secondary sexual organs.
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This gene encodes a member of a family of candidate taste receptors that are members of the G protein-coupled receptor superfamily and that are specifically expressed by taste receptor cells of the tongue and palate epithelia. These apparently intronless taste receptor genes encode a 7-transmembrane receptor protein, functioning as a bitter taste receptor. This gene is clustered with another 3 candidate taste receptor genes in chromosome 7 and is genetically linked to loci that influence bitter perception.
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Oxidized low-density lipoprotein receptor 1 (Ox-LDL receptor 1) also known as lectin-type oxidized LDL receptor 1 (LOX-1) is a protein that in humans is encoded by the OLR1 gene. LOX-1 is the main receptor for oxidized LDL on endothelial cells, macrophages, smooth muscle cells, and other cell types. But minimally oxidized LDL is more readily recognized by the TLR4 receptor, and highly oxidized LDL is more readily recognized by the CD36 receptor.
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Isoform a and isoform b sequences are different, beginning at the C-terminal regulatory domains. Studies have shown that carboxy-terminal splicing has occurred in many other transmembrane receptors, along with prostaglandin E receptor (EP3). These variants, SST2A receptor and SST2B receptor are seen in some brain and spinal cord areas in a rodent. Somatostatin receptor 2a has a shorter transcript, but is longer than somatostatin receptor 2b and has a unique C- terminus compared to Somatostatin Receptor 2b.
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The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptor (5-HT receptor) that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and its activation in the brain mediates hyperpolarisation and reduction of firing rate of the postsynaptic neuron. In humans, the serotonin 1A receptor is encoded by the HTR1A gene.
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Tropomyosin receptor kinase C (TrkC), also known as NT-3 growth factor receptor, neurotrophic tyrosine kinase receptor type 3, or TrkC tyrosine kinase is a protein that in humans is encoded by the NTRK3 gene. TrkC is the high affinity catalytic receptor for the neurotrophin NT-3 (neurotrophin-3). As such, TrkC mediates the multiple effects of this neurotrophic factor, which includes neuronal differentiation and survival. The TrkC receptor is part of the large family of receptor tyrosine kinases.
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Thyroid hormone receptor alpha (TR-alpha) also known as nuclear receptor subfamily 1, group A, member 1 (NR1A1), is a nuclear receptor protein that in humans is encoded by the THRA gene.
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Thyroid hormone receptor beta (TR-beta) also known as nuclear receptor subfamily 1, group A, member 2 (NR1A2), is a nuclear receptor protein that in humans is encoded by the THRB gene.
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Liver X receptor beta (LXR-β) is a member of the nuclear receptor family of transcription factors. LXR-β is encoded by the gene (nuclear receptor subfamily 1, group H, member 2).
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RAR-related orphan receptor beta (ROR-beta), also known as NR1F2 (nuclear receptor subfamily 1, group F, member 2) is a nuclear receptor that in humans is encoded by the RORB gene.
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Interleukin 27 receptor, alpha is a subunit of the interleukin-27 receptor. IL27RA is its human gene.
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Free fatty acid receptor 2 (FFA2) is a G-protein coupled receptor encoded by the FFAR2 gene.
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Prokineticin receptor 2 (PKR2), is a G protein-coupled receptor encoded by the PROKR2 gene in humans.
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Interleukin-23 receptor is a type I cytokine receptor. IL23R is the name of its human gene.
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PRKACB has been shown to interact with Ryanodine receptor 2 and Low affinity nerve growth factor receptor.
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The interleukin-18 receptor 1 (IL-18R1) is an interleukin receptor of the immunoglobulin superfamily. IL18R1 is its human gene. IL18R1 is also known as CDw218a (cluster of differentiation w218a). The protein encoded by this gene is a cytokine receptor that belongs to the interleukin 1 receptor family.
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The free fatty acid receptor is a G-protein coupled receptor which binds free fatty acids. There are four variants of the receptor, each encoded by a separate gene (FFAR1, FFAR2, FFAR3, FFAR4). Preliminary findings suggest that FFAR2 and FFAR3 may interact to form a FFAR2-FFAR3 receptor heteromer.
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The follicle-stimulating hormone receptor or FSH receptor (FSHR) is a transmembrane receptor that interacts with the follicle-stimulating hormone (FSH) and represents a G protein-coupled receptor (GPCR). Its activation is necessary for the hormonal functioning of FSH. FSHRs are found in the ovary, testis, and uterus.
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Dopamine receptor D5, also known as D1BR, is a protein that in humans is encoded by the DRD5 gene. It belongs to the D1-like receptor family along with the D1 receptor subtype.
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An orexin receptor antagonist is a drug that inhibits the effect of orexin by acting as a receptor antagonist of the orexin receptor. Potential applications include treatment of sleep disorders such as insomnia.
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Metoclopramide appears to bind to dopamine D2 receptors with nanomolar affinity (Ki = 28.8 nM), where it is a receptor antagonist, and is also a mixed 5-HT3 receptor antagonist/5-HT4 receptor agonist.
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G proteins are coupled to the C-terminal end of the chemokine receptor to allow intracellular signaling after receptor activation, while the N-terminal domain of the chemokine receptor determines ligand binding specificity.
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For example, PI 3-kinases may be activated by a G protein coupled receptor or receptor tyrosine kinase such as the insulin receptor. Once activated, PI 3-kinase phosphorylates PIP2 to form PIP3.
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Protease activated receptor 3 (PAR-3) also known as coagulation factor II receptor-like 2 (F2RL2) and thrombin receptor-like 2, is a protein that in humans is encoded by the F2RL2 gene.
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The testicular receptor proteins are members of the nuclear receptor family of intracellular transcription factors. There are two forms of the receptor, TR2 and TR4, each encode by a separate gene ( and respectively).
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Size of the lesion and lymph node involvement determine prognosis; thus small lesions without lymph node involvement have the best prognosis. Estrogen receptor and progesterone receptor status and HER2/neu (Human Epidermal Growth Factor Receptor 2) gene amplification need to be reported as they may affect treatment options. About 85% of all male breast cancers are estrogen receptor–positive, and 70% are progesterone receptor–positive.
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An identification of the hPG80 receptor has been the subject of several studies in recent years. However, hPG80 receptor identity remains a real issue in the scientific community. The receptor can activate a number of signaling pathways, either directly or indirectly, which is rather unusual for a receptor. This could indicate a peculiarity of this receptor and why it is difficult to identify it.
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Vasopressin V1b receptor (V1BR) also known as vasopressin 3 receptor (VPR3) or antidiuretic hormone receptor 1B is a protein that in humans is encoded by the AVPR1B (arginine vasopressin receptor 1B) gene. V1BR acts as a receptor for vasopressin. AVPR1B belongs to the subfamily of G-protein coupled receptors. Its activity is mediated by G proteins which stimulate a phosphatidylinositol- calcium second messenger system.
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Reticulon 4 receptor (RTN4R) also known as Nogo-66 Receptor (NgR) or Nogo receptor 1 is a protein which in humans is encoded by the RTN4R gene. This gene encodes the receptor for reticulon 4, oligodendrocytemyelin glycoprotein and myelin-associated glycoprotein. This receptor mediates axonal growth inhibition and may play a role in regulating axonal regeneration and plasticity in the adult central nervous system.
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The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by the SIGMAR1 gene. The σ1 receptor is a transmembrane protein expressed in many different tissue types. It is particularly concentrated in certain regions of the central nervous system.
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The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi/G0 and has enkephalins as its endogenous ligands. The regions of the brain where the δ-opioid receptor is largely expressed vary from species model to species model. In humans, the δ-opioid receptor is most heavily expressed in the basal ganglia and neocortical regions of the brain.
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The VDR gene encodes the nuclear hormone receptor for vitamin D3. This receptor also functions as a receptor for the secondary bile acid lithocholic acid. The receptor belongs to the family of trans-acting transcriptional regulatory factors and shows similarity of sequence to the steroid and thyroid hormone receptors. Downstream targets of this nuclear hormone receptor are involved principally in mineral metabolism though the receptor regulates a variety of other metabolic pathways, such as those involved in the immune response and cancer.
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RU-28362 is a synthetic androstane glucocorticoid that was developed by Roussel Uclaf. It is a selective agonist of the glucocorticoid receptor (corticoid type II receptor), but not of the mineralocorticoid receptor (corticoid type I receptor). A similar compound is dexamethasone that also selectively binds to the glucocorticoid receptor with high affinity. This is in contrast to the natural steroid hormones cortisol or corticosterone, which bind to both of the corticosteroid receptors, though they bind to the mineralocorticoid receptor with greater affinity.
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The mineralocorticoid receptor (or MR, MLR, MCR), also known as the aldosterone receptor or nuclear receptor subfamily 3, group C, member 2, (NR3C2) is a protein that in humans is encoded by the NR3C2 gene that is located on chromosome 4q31.1-31.2. MR is a receptor with equal affinity for mineralocorticoids and glucocorticoids. It belongs to the nuclear receptor family where the ligand diffuses into cells, interacts with the receptor and results in a signal transduction affecting specific gene expression in the nucleus.
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Sulprostone is an analogue of prostaglandin E2 (PGE2) that has oxytocic activity in assays of rat kidney cells and tissues. There are four known receptors which mediate various but often different cellular and tissue responses to PGE2: prostaglandin EP1 receptor, prostaglandin EP2 receptor, prostaglandin EP3 receptor, and prostaglandin EP4 receptor. Sulprosotone binds to and activates the prostaglandin EP3 receptor with far greater efficacy than the other PGE2 receptors and also has the advantage of being relatively resistant, compared with PGE2, to becoming metabolically degraded. It is listed as a comparatively weak receptor agonist of the prostaglandin EP1 receptor.
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Levorphanol acts predominantly as an agonist of the μ-opioid receptor (MOR), but is also an agonist of the δ-opioid receptor (DOR), κ-opioid receptor (KOR), and the nociceptin receptor (NOP), as well as an NMDA receptor antagonist and a serotonin-norepinephrine reuptake inhibitor (SNRI). Levorphanol, similarly to certain other opioids, also acts as a glycine receptor antagonist and GABA receptor antagonist at very high concentrations. Levorphanol is 6 to 8 times as potent as morphine at the MOR. Relative to morphine, levorphanol lacks complete cross-tolerance and possesses greater intrinsic activity at the MOR.
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Relaxin/insulin-like family peptide receptor 3, also known as RXFP3, is a human G-protein coupled receptor.
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Relaxin/insulin-like family peptide receptor 4, also known as RXFP4, is a human G-protein coupled receptor.
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Interleukin-20 receptor is a type II cytokine receptor. It is a heterodimer of α and β subunits.
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H2 receptor blockers lead to roughly a 40% improvement. H2 receptor antagonists are named using the suffix "-tidine".
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Bradykinin receptor B2 is a G-protein coupled receptor for bradykinin, encoded by the BDKRB2 gene in humans.
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Interleukin 6 receptor (IL6R) also known as CD126 (Cluster of Differentiation 126) is a type I cytokine receptor.
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MED24 has been shown to interact with Estrogen receptor alpha, Cyclin-dependent kinase 8, Calcitriol receptor and BRCA1.
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In response to bile acids, mouse Mafg gene is induced by the nuclear receptor, FXR (Farnesoid X receptor).
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GRB14 has been shown to interact with Epidermal growth factor receptor, Fibroblast growth factor receptor 1 and TNKS2.
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It is an important mediator involved in many cytokine induced immune and inflammatory responses. This gene along with interleukin 1 receptor, type II (IL1R2), interleukin 1 receptor-like 2 (IL1RL2), and interleukin 1 receptor-like 1 (IL1RL1) form a cytokine receptor gene cluster in a region mapped to chromosome 2q12.
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Angiotensin II receptor type 1 or AT1 receptor is the best characterized angiotensin receptor. It has vasopressor effects and regulates aldosterone secretion. It is an important effector controlling blood pressure and volume in the cardiovascular system. Angiotensin II receptor antagonists are drugs indicated for hypertension, diabetic nephropathy and congestive heart failure.
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Decoy receptor 3 (Dcr3), also known as tumor necrosis factor receptor superfamily member 6B (TNFRSF6B), TR6 and M68, is a soluble protein of the tumor necrosis factor receptor superfamily which inhibits Fas ligand-induced apoptosis.
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N-formyl peptide receptor 3 (FPR3) is a receptor protein that in humans is encoded by the FPR3 gene.
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It is believed that senecavirus internalizes by receptor-mediated internalization, but as yet no host receptor has been identified.
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Norgestomet is a progestogen. In addition to the progesterone receptor, it possesses weak (micromolar) affinity for the glucocorticoid receptor.
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The FFAR2–FFAR3 receptor heteromer is a receptor heteromer consisting of free fatty acid receptors, FFAR2 and FFAR3 protomers.
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MED16 has been shown to interact with Thyroid hormone receptor alpha, Estrogen receptor alpha and Cyclin-dependent kinase 8.
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Forasartan, otherwise known as the compound SC-52458, is a nonpeptide angiotensin II receptor antagonist (ARB, AT1 receptor blocker).
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AB-PICA is a potent agonist for the CB1 receptor (EC50 = 12 nM) and CB2 receptor (EC50 = 12 nM).
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Her lab identified a particular receptor, the aryl hydrocarbon receptor (AhR), which connects environmental stimuli and the immune system.
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The alpha-3 beta-2 nicotinic receptor, also known as the α3β2 receptor, is a type of nicotinic acetylcholine receptor, consisting of α3 and β2 subunits. It occurs alongside the more common α3β4 nicotinic receptor in autonomic ganglia, and as an facilitatory presynaptic autoreceptor at the neuromuscular junction (NMJ). At the NMJ, it is involved in upregulation of ACh release during high- frequency stimulation. Nicotine, a component of tobacco, a common stimulate of the receptor has been found to increase the concentration of this receptor.
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A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ligand-gated ion channel of the major inhibitory neurotransmitter γ-aminobutyric acid (GABA). They are closely related and similar to GABAA receptor antagonists. The effects of GABAA receptor NAMs are functionally the opposite of those of GABAA receptor positive allosteric modulators (PAMs) like the benzodiazepines, barbiturates, and ethanol (alcohol). Non-selective GABAA receptor NAMs can produce a variety of effects including convulsions, neurotoxicity, and anxiety, among others.
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While the effect of editing on protein function is unknown, the developmental increase in editing does correspond to changes in function of the GABAA receptor. GABA binding leads to chloride channel activation, resulting in rapid increase in concentration of the ion. Initially, the receptor is an excitatory receptor, mediating depolarisation (efflux of Cl− ions) in immature neurons before changing to an inhibitory receptor, mediating hyperpolarisation (influx of Cl− ions) later on. GABAA converts to an inhibitory receptor from an excitatory receptor by the upregulation of KCC2 cotransporter.
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The three domains are: membrane fusion, esterase, and receptor binding domains. The different HEs enzyme activities include: receptor binding activity, receptor hydrolysis (esterase) activity, and membrane fusion activity. The receptor binding activity involve the attachment of HEs to N-acetyl-9-O-acetylneuraminic acid (9-O-Ac- Neu5Ac) of glycolipids and glycoproteins and in turn serve as viral receptor. Receptor hydrolysis (esterase) activity allows virus particles to escape the infected cell by removing an acetyl group from the C9 position of terminal 9-O-Ac-Neu5Ac residues.
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Many tiny hair-like cilia protrude from the olfactory receptor cell's dendrite into the mucus covering the surface of the olfactory epithelium. The surface of these cilia is covered with olfactory receptors, a type of G protein-coupled receptor. Each olfactory receptor cell expresses only one type of olfactory receptor (OR), but many separate olfactory receptor cells express ORs which bind the same set of odors. The axons of olfactory receptor cells which express the same OR converge to form glomeruli in the olfactory bulb.
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Antagonists were thought to turn "off" that response by 'blocking' the receptor from the agonist. This definition also remains in use for physiological antagonists, substances that have opposing physiological actions, but act at different receptors. For example, histamine lowers arterial pressure through vasodilation at the histamine H1 receptor, while adrenaline raises arterial pressure through vasoconstriction mediated by alpha-adrenergic receptor activation. Our understanding of the mechanism of drug-induced receptor activation and receptor theory and the biochemical definition of a receptor antagonist continues to evolve.
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The two-state model of receptor activation has given way to multistate models with intermediate conformational states. The discovery of functional selectivity and that ligand-specific receptor conformations occur and can affect interaction of receptors with different second messenger systems may mean that drugs can be designed to activate some of the downstream functions of a receptor but not others. This means efficacy may actually depend on where that receptor is expressed, altering the view that efficacy at a receptor is receptor-independent property of a drug.
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The molecular target of the active metabolite of ADP receptor inhibitors is the P2Y12 receptor. P2Y12 receptor is a G-coupled receptor and is activated by adenosine diphosphate. ADP binds to the P2Y12 receptor that leads to inhibition of adenyl cyclase and thereby decreases the intracellular levels of cAMP. This reduction of cAMP reduces phosphorylation of vasodilator stimulated phosphoprotein that leads to the activation of the glycoprotein IIb/IIIa receptors.
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Interleukin 21 receptor is a type I cytokine receptor. IL21R is its human gene. The protein encoded by this gene is a cytokine receptor for interleukin 21 (IL21). It belongs to the type I cytokine receptors, and has been shown to form a heterodimeric receptor complex with the common gamma-chain, a receptor subunit also shared by the receptors for interleukin 2 (IL2), interleukin 7 (IL7) and interleukin 15 (IL15).
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Interleukin-1 receptor (IL-1R) is a cytokine receptor which binds interleukin 1. Two forms of the receptor exist. The type I receptor is primarily responsible for transmitting the inflammatory effects of interleukin-1 (IL-1) while type II receptors may act as a suppressor of IL-1 activity by competing for IL-1 binding. Also opposing the effects of IL-1 is the IL-1 receptor antagonist (IL-1RA).
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Vasopressin receptor 2 function has been shown to be deleteriously effected by point mutations in its gene. Some of these mutations, when expressed, cause the receptor to remain in the cytosol. An approach to rescue receptor function utilizes pharmacoperones or molecular chaperones, which are typically small molecules that rescue misfolded proteins to the cell surface. These interact with the receptor to restore cognate receptor function devoid of antagonist or agonist activity.
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Endocytosis is triggered when a specific receptor is activated in Receptor- mediated endocytosis. The function of receptor-mediated endocytosis is diverse. It is widely used for the specific uptake of certain substances required by the cell (examples include LDL via the LDL receptor or iron via transferrin). The role of receptor-mediated endocytosis is well recognized up take downregulation of transmembrane signal transduction but can also promote sustained signal transduction.
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Interleukin-28 receptor is a type II cytokine receptor found in skin cells. It binds interleukin-28 A and B as well as interleukin 29. It consists of an α and shares a common β subunit with the interleukin-10 receptor. Binding to the interleukin-28 receptor is important for fighting infection.
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The exact mechanism of the action of general anaesthetics has not been delineated. Sevoflurane acts as a positive allosteric modulator of the GABAA receptor in electrophysiology studies of neurons and recombinant receptors. However, it also acts as an NMDA receptor antagonist, potentiates glycine receptor currents, and inhibits nAChR and 5-HT3 receptor currents.
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The apelin receptor (also known as the APJ receptor) is a G protein-coupled receptor which binds apelin and Apela/ELABELA/Toddler.Chng, S. C., Ho, L., Tian, J., & Reversade, B. (2013). ELABELA: a hormone essential for heart development signals via the apelin receptor. Developmental Cell, 27(6), 672–680. doi:10.1016/j.devcel.2013.11.
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In this case, the receptor is a carbon nanotube. Note that while physical mixtures of a primary hydrogen spillover source and a secondary receptor demonstrate moderate storage capacity, adding a bridge to improve the contact between the support metal and the receptor serves to double or triple hydrogen storage capacity on the receptor.
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Hyper-IL-6 is a designer cytokine, which was generated by the German biochemist Stefan Rose-John. Hyper-IL-6 is a fusion protein of the four- helical cytokine Interleukin-6 and the soluble Interleukin-6 receptor which are covalently linked by a flexible peptide linker. Interleukin-6 on target cells binds to a membrane bound Interleukin-6 receptor. The complex of Interleukin-6 and the Interleukin-6 receptor associate with a second receptor protein called gp130, which dimerises and initiates intracellular signal transduction. Gp130 is expressed on all cells of the human body whereas the Interleukin-6 receptor is only found on few cells such as hepatocytes and some leukocytes. Neither Interleukin-6 nor the Interleukin-6 receptor have a measurable affinity for gp130. Therefore, cells, which only express gp130 but no Interleukin-6 receptor are not responsive to Interleukin-6. It was found, however, that the membrane-bound Interleukin-6 receptor can be cleaved from the cell membrane generating a soluble Interleukin-6 receptor. The soluble Interleukin-6 receptor can bind the ligand Interleukin-6 with similar affinity as the membrane-bound Interleukin-6 receptor and the complex of Interleukin-6 and the soluble Interleukin-6 receptor can bind to gp130 on cells, which only express gp130 but no Interleukin-6 receptor.
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In 1983, evidence for a 5-HT1-like receptor was first found. Ten years later, 5-HT7 receptor was cloned and characterized. It has since become clear that the receptor described in 1983 is 5-HT7.
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Ephrin receptors make up the largest subgroup of the receptor tyrosine kinase (RTK) family. The ephrin receptor encoded by this gene lacks the kinase activity of most receptor tyrosine kinases and binds to ephrin-B ligands.
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Discoidin domain-containing receptor 2, also known as CD167b (cluster of differentiation 167b), is a protein that in humans is encoded by the DDR2 gene. Discoidin domain-containing receptor 2 is a receptor tyrosine kinase (RTK).
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In the mid-1990s, Gustafsson's research group at the Karolinska Institutet discovered estrogen receptor-beta, which plays a pivotal role in the function of the brain, lungs, and immune system. Today, drugs are being developed to stimulate that receptor to battle a number of diseases, including breast, prostate and lung cancers. In some instances, the abnormal cell division that creates cancerous tumors can be slowed down or stopped by stimulating the receptor. Additional discoveries include early demonstration of the three-domain structure of nuclear receptors, specific binding of nuclear receptors to DNA, discovery of steroid response element, cloning of the first nuclear receptor fragment, first determination a 3-D structure of a nuclear receptor (the DNA binding domain of the glucocorticoid receptor), discovery of the first physiological ligand of a nuclear receptor (fatty acids for the peroxisome proliferator activated receptor alpha), discovery of liver X receptor beta (LXRβ), discovery of estrogen receptor beta (ERβ) and unravelling of some of their functions.
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Proteins may be metabolized or the receptor can be recycled. Use of long-acting agonists will downregulate the receptor population.
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Proteins may be metabolized or the receptor can be recycled. Use of long-acting agonists will downregulate the receptor population.
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Activity of this protein is also modulated by binding to the Wnt co-receptor LDL-receptor related protein 6 (LRP6).
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Gamma-aminobutyric acid (GABA) B receptor, 1 (GABAB1), is a G-protein coupled receptor subunit encoded by the GABBR1 gene.
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Flupirtine is a selective neuronal potassium channel opener that also has indirect NMDA receptor antagonist and GABAA receptor modulatory properties.
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The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it.
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The adenosine A3 receptor, also known as ADORA3, is an adenosine receptor, but also denotes the human gene encoding it.
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EPH receptor A3 (ephrin type-A receptor 3) is a protein that in humans is encoded by the EPHA3 gene.
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EPH receptor A2 (ephrin type-A receptor 2) is a protein that in humans is encoded by the EPHA2 gene.
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Moreover, GLP2 prevents intestinal hypoplasia resulting from total parenteral nutrition. GLP2R, a G protein-coupled receptor superfamily member is expressed in the gut and closely related to the glucagon receptor (GCGR) and the receptor for GLP1 (GLP1R).
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Its values are 19 nM for the α1-adrenergic receptor, 4,945 nM for the α2-adrenergic receptor, and 70 nM for the serotonin 5-HT2A receptor. Perlapine is closely related to clotiapine, clozapine, fluperlapine, loxapine, and tilozepine.
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Binding interaction between NGF and the TrkA receptor facilitates receptor dimerization and tyrosine residue phosphorylation of the cytoplasmic tail by adjacent Trk receptors. Trk receptor phosphorylation sites operate as Shc adaptor protein docking sites, which undergo phosphorylation by the TrkA receptor Once the cytoplasmic adaptor protein (Shc) is phosphorylated by the receptor cytoplasmic tail, cell survival is initiated through several intracellular pathways. One major pathway leads to the activation of the serine/threonine kinase, Akt. This pathway begins with the Trk receptor complex-recruitment of a second adaptor protein called growth factor-receptor bound protein-2 (Grb2) along with a docking protein called Grb2-associated Binder-1 (GAB1).
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As such, due to its high affinity for the σ1 receptor, (+)-alazocine can be used to distinguish between the two sigma receptor subtypes in scientific research, for instance in radioligand binding assays. Taken together, (–)-alazocine is a selective partial agonist of the κ-opioid receptor, antagonist of the μ-opioid receptor, and to a far lesser extent agonist of the δ-opioid receptor with very low affinity for the sigma receptors, while (+)-alazocine is a selective agonist of the sigma σ1 receptor and to a lesser (~10-fold) extent antagonist of the NMDA receptor with low affinity for the opioid and sigma σ2 receptors.
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IGF-1 binds to at least two cell surface receptor tyrosine kinases: the IGF-1 receptor (IGF1R), and the insulin receptor. Its primary action is mediated by binding to its specific receptor, IGF1R, which is present on the surface of many cell types in many tissues. Binding to the IGF1R initiates intracellular signaling. IGF-1 is one of the most potent natural activators of the AKT signaling pathway, a stimulator of cell growth and proliferation, and a potent inhibitor of programmed cell death . The IGF-1 receptor seems to be the "physiologic" receptor because it binds IGF-1 with significantly higher affinity than insulin receptor does.
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The studies cited above lead to the eventual cloning of the human Formyl peptide receptor 1, a G protein coupled receptor that binds fMLF and other formylated oligopeptides to mediate their stimulatory actions on human and rabbit neutrophils. Subsequently, Formyl peptide receptor 2 and Formyl peptide receptor 3 were also cloned based on the similarities in their amino acid sequence to that of formyl peptide receptor 1. Formyl peptide receptors 2 and 3 have very different abilities to bind and respond to formylated oligopeptides including fMLF compared to formyl peptide receptor 1 and compared to each other and have very different functions than those of formyl peptide receptor 1.
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Purification of the receptor further verified its existence. The first attempt to purify the receptor involved the use of a novel opioid receptor antagonist called chlornaltrexamine that was demonstrated to bind to the opioid receptor. Caruso later purified the detergent-extracted component of rat brain membrane that eluted with the specifically bound 3H-chlornaltrexamine.
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TDBzcholine is able to bind to the nicotinic acetylcholine receptor. Once TDBzcholine is bound to the receptor, TDBzcholine can be activated by exposing the sample to UV light. This led to formation of a highly reactive carbene radical that can react with amino acid residues in the receptor and become covalently bound to the receptor.
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The Taghert group also demonstrated that PDF signaling influences pacemaker cell synchronicity through PER regulation, identified the PDF receptor, and identified critical PDF receptor signaling components. They have shown that PDF receptor signals differently in different pacemaker groups, and that PDF receptor signaling interact with signals from Cryptochrome (CRY) to help sustain clock rhythmicity.
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The distinctive taste of chalk has been identified as the calcium component of that substance. In 2008, geneticists discovered a calcium receptor on the tongues of mice. The CaSR receptor is commonly found in the gastrointestinal tract, kidneys, and brain. Along with the "sweet" T1R3 receptor, the CaSR receptor can detect calcium as a taste.
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In the field of molecular biology, the pregnane X receptor (PXR), also known as the steroid and xenobiotic sensing nuclear receptor (SXR) or nuclear receptor subfamily 1, group I, member 2 (NR1I2) is a protein that in humans is encoded by the NR1I2 (nuclear Receptor subfamily 1, group I, member 2) gene.Entrez result for NR1I2.
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Kinase insert domain receptor (KDR, a type IV receptor tyrosine kinase) also known as vascular endothelial growth factor receptor 2 (VEGFR-2) is a VEGF receptor. KDR is the human gene encoding it. KDR has also been designated as CD309 (cluster of differentiation 309). KDR is also known as Flk1 (Fetal Liver Kinase 1).
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Another receptor can also bind IgA, although it has higher affinity for another antibody called IgM. This receptor is called the Fc- alpha/mu receptor (Fcα/μR) and is a type I transmembrane protein. With one Ig- like domain in its extracellular portion, this Fc receptor is also a member of the immunoglobulin superfamily.
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The signalling of the D1–D2 receptor heteromer is distinct from that of the parent receptor monomers. It comprises Gq/11 coupling, phospholipase C activation, intracellular calcium release from inositol trisphosphate receptor-sensitive stores, CaMKII activation and BDNF production. In comparison, signalling of the homologous D5–D2 receptor heteromer involves the influx of extracellular calcium.
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Odorant receptor genes also play a major role in odor identification. Expression in olfactory receptor neurons has been confirmed for a limited subset of the huge number of odorant receptor genes. Genetic analysis shows that odorant receptor neurons express only one type of odorant receptor gene. It is hypothesized that different odors activate different receptors, and genetic regulation of odorant receptors results in the diversity for olfactory receptor neurons and this allows the capacity of olfactory systems to detect and encode a wide range of complex and novel odors in the environment.
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Upon binding of LH to the external part of the membrane spanning receptor, a transduction of the signal takes place that activates the G protein that is bound to the receptor internally. With LH attached, the receptor shifts conformation and thus mechanically activates the G protein, which detaches from the receptor and activates the cAMP system. It is believed that a receptor molecule exists in a conformational equilibrium between active and inactive states. The binding of LH (or CG) to the receptor shifts the equilibrium between active and inactive receptors.
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The AR translocates to the nucleus where dimerization, DNA binding, and the recruitment of coactivators occur. Target genes are transcribed (mRNA) and translated into proteins. The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone in the cytoplasm and then translocating into the nucleus. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor.
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Peroxisome proliferator-activated receptor alpha (PPAR-alpha), also known as NR1C1 (nuclear receptor subfamily 1, group C, member 1), is a nuclear receptor protein that in humans is encoded by the PPARA gene. Together with peroxisome proliferator-activated receptor delta and peroxisome proliferator-activated receptor gamma, PPAR-alpha is part of the subfamily of peroxisome proliferator-activated receptors. It was the first member of the PPAR family to be cloned in 1990 by Stephen Green and has been identified as the nuclear receptor for a diverse class of rodent hepatocarcinogens that causes proliferation of peroxisomes.
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In the context of aftertaste, the combination of both receptor-dependent and receptor-independent processes have been proposed to explain the signal transduction mechanisms for foods with distinct aftertastes, particularly those that are bitter. The receptor-dependent process is the same as what was described above. However, the receptor-independent process involves the diffusion of bitter, amphiphilic chemicals like quinine across the taste receptor cell membranes. Once inside the taste receptor cell, these compounds have been observed to activate intracellular G-proteins and other proteins that are involved in signaling pathways routed to the brain.
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Selective CB1 agonists may be used to isolate the effects of the receptor from the CB2 receptor, as most cannabinoids and endocannabinoids bind to both receptor types. CB1 selective antagonists are used for weight reduction and smoking cessation (see Rimonabant). A substantial number of antagonists of the CB1 receptor have been discovered and characterized. TM38837 has been developed as a CB1 receptor antagonist that is restricted to targeting only peripheral CB1 receptors.
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When only the transmembrane regions of the receptors are considered, however, the amino acid similarity between the two receptor subtypes is approximately 68%. The amino acid sequence of the CB2 receptor is less highly conserved across human and rodent species as compared to the amino acid sequence of the CB1 receptor. Based on computer modeling, ligand interactions with CB2 receptor residues S3.31 and F5.46 appears to determine differences between CB1 and CB2 receptor selectivity.
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PTPrho is also upregulated in estrogen receptor alpha positive breast tumor samples versus estrogen receptor alpha negative tumor samples. The authors evaluated 560 selected genes by real-time quantitative reverse transcription-polymerase chain reaction (RT- PCR) in estrogen receptor alpha positive tissue and compared it to estrogen receptor alpha negative tissue, and found that PTPrho(PTPRT) was upregulated in the estrogen receptor alpha tissue, suggesting a non-tumor suppressor role for PTPrho.
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JTC-801 is an opioid analgesic drug used in scientific research. JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor. This was the fourth opioid receptor to be discovered and is still the least understood. The nociceptin receptor has complex effects which are involved in many processes involved in pain and inflammation responses, and activation of this receptor can either increase or reduce pain depending on dose.
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Each bind to a specific type II receptor-ligand complex. Despite the large amount of processes that these ligands regulate, they all operate through essentially the same pathway: A ligand binds to a Type two receptor, which recruits and trans-phosphorylate a type I receptor. The type I receptor recruits a receptor regulated SMAD (R-SMAD) which it phosphorylates. The RSMAD then translocates to the nucleus where it functions as a transcription factor.
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The Gq-coupled membrane estrogen receptor (Gq-mER) is a G protein-coupled receptor present in the hypothalamus that has not yet been cloned. It is a membrane-associated receptor that is Gq-coupled to a phospholipase C–protein kinase C–protein kinase A (PLC–PKC–PKA) pathway. The receptor has been implicated in the control of energy homeostasis. Gq-mER is bound and activated by estradiol, and is a putative membrane estrogen receptor (mER).
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A ligand produced by one cell binds to a receptor in the extracellular region of another cell, inducing a conformational change in the receptor. The shape of the cytoplasmic domain of the receptor changes, and the receptor acquires enzymatic activity. The receptor then catalyzes reactions that phosphorylate other proteins, activating them. A cascade of phosphorylation reactions eventually activates a dormant transcription factor or cytoskeletal protein, thus contributing to the differentiation process in the target cell.
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IGF-1 is closely related to a second protein called "IGF-2". IGF-2 also binds the IGF-1 receptor. However, IGF-2 alone binds a receptor called the "IGF-2 receptor" (also called the mannose-6 phosphate receptor). The insulin-like growth factor-II receptor (IGF2R) lacks signal transduction capacity, and its main role is to act as a sink for IGF-2 and make less IGF-2 available for binding with IGF-1R.
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The syncytin-1 receptor is the Na-dependent amino acid transporter 2 (ASCT2 or SLC1A5). This receptor places syncytin-1 in a large viral interference group called retroviral mammalian type D receptor (RDR) interference group. Syncytin-1 has been shown to interfere with viral infection in-vitro by RDR interference group member spleen necrosis virus. Syncytin-1 can also recognize ASCT1 or SLC1A4, but this receptor is not a receptor for the RDR interference group.
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Interleukin 9 receptor (IL9R) also known as CD129 (Cluster of Differentiation 129) is a type I cytokine receptor. IL9R also denotes its human gene. The protein encoded by this gene is a cytokine receptor that specifically mediates the biological effects of interleukin 9 (IL9). The functional IL9 receptor complex requires this protein as well as the interleukin 2 receptor, gamma (IL2RG), a common gamma subunit shared by the receptors of many different cytokines.
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Interleukin 13 receptor, alpha 1, also known as IL13RA1 and CD213A1 (cluster of differentiation 213A1), is a human gene. The protein encoded by this gene is a subunit of the interleukin 13 receptor. This subunit forms a receptor complex with IL4 receptor alpha, a subunit shared by IL13 and IL4 receptors. This subunit serves as a primary IL13-binding subunit of the IL13 receptor, and may also be a component of IL4 receptors.
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BD1018 or (S)-2-[2-(3,4-dichlorophenyl)ethyl]octahydropyrrolo[1,2-a]pyrazine is a selective sigma receptor ligand, with a reported binding affinity of Ki = 5 ± 0.7 nM for the sigma-1 receptor and approximately 10 times selectivity over the sigma-2 receptor. Unlike its enantiomer, BD1031, BD1018 acts as a sigma receptor antagonist. Consistent with other reported sigma receptor antagonists, BD1018 decreases the behavioural toxicity of cocaine in Swiss Webster mice.
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Sphingosine-1-phosphate receptor 3 also known as S1PR3 is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P). Hence this receptor is also known as S1P3.
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Sphingosine-1-phosphate receptor 5 also known as S1PR5 is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P). Hence this receptor is also known as S1P5.
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Sphingosine-1-phosphate receptor 4 also known as S1PR4 is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P). Hence this receptor is also known as S1P4.
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The FSH receptor can also activate the extracellular signal-regulated kinases (ERK). In a feedback mechanism, these activated kinases phosphorylate the receptor. The longer the receptor remains active, the more kinases are activated, the more receptors are phosphorylated.
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The AH receptor is an ancient receptor, and its many functions have been revealed only recently.Hahn, Mark E.; Karchner, Sibel I. (2011). "Structural and Functional Diversification of AHRs during Metazoan Evolution". The AH Receptor in Biology and Toxicology.
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Mas-related G-protein coupled receptor member G (MRGG) also known as G-protein coupled receptor 169 (GPR169) is a protein that in humans is encoded by the MRGPRG gene. MRGG is an orphan G-protein coupled receptor.
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Receptor tyrosine kinases are part of the larger family of protein tyrosine kinases, encompassing the receptor tyrosine kinase proteins which contain a transmembrane domain, as well as the non-receptor tyrosine kinases which do not possess transmembrane domains.
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Nociceptin acts at the Nociceptin receptor (NOP receptor) formerly known as ORL1. Nociceptin is the first example of reverse pharmacology; the NOP receptor was discovered before the endogenous ligand which was discovered by two separate groups in 1995.
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The muscarinic acetylcholine receptor M2, also known as the cholinergic receptor, muscarinic 2, is a muscarinic acetylcholine receptor that in humans is encoded by the CHRM2 gene. Multiple alternatively spliced transcript variants have been described for this gene.
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The following are all μ-opioid receptor (MOR) antagonists or inverse agonists. Many of them also bind to the κ-opioid receptor (KOR) and/or δ-opioid receptor (DOR), where they variously behave as antagonists and/or agonists.
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LAAM acts as a μ-opioid receptor agonist. It also acts as a potent, noncompetitive α3β4 neuronal nicotinic acetylcholine receptor antagonist.
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Free fatty acid receptor 3 (FFA3) is a G-protein coupled receptor that in humans is encoded by the FFAR3 gene.
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Pregnanolone is a positive allosteric modulator of the GABAA receptor, as well as a negative allosteric modulator of the glycine receptor.
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Interleukin 12 receptor is a type I cytokine receptor, binding interleukin 12. It consists of beta 1 and beta 2 subunits.
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Cartoon representation of the human hormone estrogen receptor DBD. DNA = orange and blue. DBD of estrogen receptor = white. Zinc atoms = green.
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They are SRIs and litoxetine is also a 5-HT3 receptor antagonist while lubazodone is also a 5-HT2A receptor antagonist.
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This history has led to contemporary research into drugs which are H3 receptor antagonist and which affect the Histamine H4 receptor.
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This gene encodes for a new transmembrane receptor and it is proposed that this receptor is an upstream regulator of SHH.
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2-Chloro-N6-cyclopentyladenosine (CCPA) is a specific receptor agonist for the Adenosine A1 receptor. It is similar to N6-cyclopentyladenosine.
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WHIM syndrome results from autosomal dominant mutations in the gene for the chemokine receptor, CXCR4, resulting in a carboxy-terminus truncation of the receptor of between ten and 19 residues. The gene mutant is located on 2q21. The truncation of the receptor protein results in the inability of downregulation after stimulation. Thus, the receptor remain in an activated state.
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Dopamine receptor D3 is a protein that in humans is encoded by the DRD3 gene. This gene encodes the D3 subtype of the dopamine receptor. The D3 subtype inhibits adenylyl cyclase through inhibitory G-proteins. This receptor is expressed in phylogenetically older regions of the brain, suggesting that this receptor plays a role in cognitive and emotional functions.
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Peroxisome proliferator-activated receptor beta or delta (PPAR-β or PPAR-δ), also known as NR1C2 (nuclear receptor subfamily 1, group C, member 2) is a nuclear receptor that in humans is encoded by the PPARD gene. This gene encodes a member of the peroxisome proliferator-activated receptor (PPAR) family. It was first identified in Xenopus in 1993.
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Issue 6. pp. 658-672. The medication does interact with the glucocorticoid receptor however; it has about 4% of the affinity of dexamethasone for the rabbit glucocorticoid receptor. But it acts as a partial agonist of the receptor and has no greater efficacy than progesterone in activating the receptor and eliciting associated gene expression in vitro.
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Lipid rafts have been found by researchers to be involved in many signal transduction processes, such as Immunoglobulin E signalling, T cell antigen receptor signalling, B cell antigen receptor signalling, EGF receptor signalling, insulin receptor signalling and so on. In order to illustrate these principles, detailed examples of signalling pathways that involve lipid rafts are described below.
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This somewhat peculiar behavior can be attributed to B. dahlbomii's ability to rely on a specific receptor system, the L-receptor system, to perform achromatic contrast and detect and distinguish the color red. Research on the B. dahlbomii L-receptor receptor system has forced experts to partially change the ways they think about bumblebee light/color sensitivity.
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SB-204741 is a drug which acts as a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 135x selectivity over the closely related 5-HT2C receptor, and even higher over the 5-HT2A receptor and other targets. It is used in scientific research for investigating the functions of the 5-HT2B receptor.
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Ligand binding causes two reactions: # Dimerization of two monomeric receptor kinases or stabilization of a loose dimer. Many ligands of receptor tyrosine kinases are multivalent. Some tyrosine receptor kinases (e.g., the platelet-derived growth factor receptor) can form heterodimers with other similar but not identical kinases of the same subfamily, allowing a highly varied response to the extracellular signal.
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GABOB is a GABA receptor agonist. It has two stereoisomers, and shows stereoselectivity in its actions. Specifically, (R)-(–)-GABOB is a moderate-potency agonist of the GABAB receptor, while (S)-(+)-GABOB is a partial agonist of the GABAB receptor and an agonist of the GABAA receptor. (S)-(+)-GABOB is around twice as potent an anticonvulsant as (R)-(–)-GABOB.
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Simplified model of NMDAR activation and various types of NMDAR blockers. The NMDA receptor is an ionotropic receptor that allows for the transfer of electrical signals between neurons in the brain and in the spinal column. For electrical signals to pass, the NMDA receptor must be open. To remain open, glutamate and glycine must bind to the NMDA receptor.
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BD1060 or N-[2-(3,4-dichlorophenyl)ethyl]-1-pyrrolidineethanamine is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 3 ± 0.1 nM for the sigma-1 receptor and greater than 50 times selectivity over the sigma-2 receptor. Like other sigma receptor antagonists, pretreating Swiss Webster mice with BD1060 significantly reduces the behavioral toxicity of cocaine.
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Or83b, also known as Orco (short for "odorant receptor co-receptor"), is an odorant receptor and the corresponding gene that encodes it. The odorant receptor Or83b is not exclusively expressed in insects. Though its actual function is still a mystery, the broadly expressed Or83b has been conserved across highly divergent insect populations across 250 million years of evolution.
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IL-31RA was originally referred to as GLM-R (for gp130-like monocyte receptor) or GPL (for gp130-like receptor). Although the IL-31 receptor complex lacks gp130, IL-31RA has similarities to gp130 like its previous descriptors suggest.
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Herstatin is an autoinhibitor of the ErbB family, which binds to RTKs and blocks receptor dimerization and tyrosine phosphorylation. CHO cells transfected with herstatin resulted in reduced receptor oligomerization, clonal growth and receptor tyrosine phosphorylation in response to EGF.
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DHEA has been found to directly act on several neurotransmitter receptors, including acting as a positive allosteric modulator of the NMDA receptor, as a negative allosteric modulator of the GABAA receptor, and as an agonist of the σ1 receptor.
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PDGFRA, i.e. platelet-derived growth factor receptor A, also termed PDGFRα, i.e. platelet-derived growth factor receptor α, or CD140a i.e. Cluster of Differentiation 140a, is a receptor located on the surface of a wide range of cell types.
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A co-receptor is a cell surface receptor that binds a signalling molecule in addition to a primary receptor in order to facilitate ligand recognition and initiate biological processes, such as entry of a pathogen into a host cell.
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There appear to be at least three distinct receptor complexes that amylin binds to with high affinity. All three complexes contain the calcitonin receptor at the core, plus one of three receptor activity-modifying proteins, RAMP1, RAMP2, or RAMP3.
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TRPP (transient receptor potential polycystic) is a family of transient receptor potential ion channels which when mutated can cause polycystic kidney disease.
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Gamma-aminobutyric acid (GABA) B receptor, 2 (GABAB2) is a G-protein coupled receptor subunit encoded by the GABBR2 gene in humans.
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The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as endogenous ligand.
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It has also been shown to function as a 5-HT1A receptor partial agonist and 5-HT2A and 5-HT2B receptor antagonist.
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Bazedoxifene is a selective estrogen receptor modulator (SERM), or a mixed agonist and antagonist of the estrogen receptor (ER) in different tissues.
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Second, it serves as an adaptor protein to aid the receptor to the clathrin-dependent endocytosis machinery (to induce receptor- mediated endocytosis).
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DHEA-S has also been found to inhibit the TRPV1 and TRPC5 transient receptor potential channels and to inhibit the P2X receptor.
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The glutamate receptor, metabotropic 1, also known as GRM1, is a human gene which encodes the metabotropic glutamate receptor 1 (mGluR1) protein.
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Interleukin 15 receptor, alpha subunit is a subunit of the interleukin 15 receptor that in humans is encoded by the IL15RA gene.
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The cAMP signal transduction contains 5 main characters: stimulative hormone receptor (Rs) or inhibitory hormone receptor (Ri); stimulative regulative G-protein (Gs) or inhibitory regulative G-protein (Gi); adenylyl cyclase; protein kinase A (PKA); and cAMP phosphodiesterase. Stimulative hormone receptor (Rs) is a receptor that can bind with stimulative signal molecules, while inhibitory hormone receptor (Ri) is a receptor that can bind with inhibitory signal molecules. Stimulative regulative G-protein is a G-protein linked to stimulative hormone receptor (Rs), and its α subunit upon activation could stimulate the activity of an enzyme or other intracellular metabolism. On the contrary, inhibitory regulative G-protein is linked to an inhibitory hormone receptor, and its α subunit upon activation could inhibit the activity of an enzyme or other intracellular metabolism.
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The testicular receptor 2 (TR2) also known as NR2C1 (nuclear receptor subfamily 2, group C, member 1) is protein that in humans is encoded by the NR2C1 gene. TR2 is a member of the nuclear receptor family of transcription factors.
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Uracil nucleotide/cysteinyl leukotriene receptor is a G protein-coupled receptor that in humans is encoded by the GPR17 gene located on chromosome 2 at position q21. The actual activating ligands for and some functions of this receptor are disputed.
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It is chemotactic for thymocytes, macrophages, and dendritic cells. CCL25 elicits its effects by binding to the chemokine receptor CCR9.Zaballos et al., Identification of the orphan chemokine receptor GPR-9-6 as CCR9, the receptor for the chemokine TECK.
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The N-Acetylglucosamine (GlcNAc) receptor has been recently found to interact and bind with vimentins at the cell surface. Research indicates that the GlcNAc receptor can therefore be used to target vimentin-expressing cells for gene delivery via receptor-mediated endocytosis.
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The G protein-coupled bile acid receptor 1 (GPBAR1) also known G-protein coupled receptor 19 (GPCR19), membrane-type receptor for bile acids (M-BAR) or TGR5 as is a protein that in humans is encoded by the GPBAR1 gene.
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The prolactin-releasing peptide receptor (PrRPR) also known as G-protein coupled receptor 10 (GPR10) is a protein that in humans is encoded by the PRLHR gene. PrRPR is a G-protein coupled receptor that binds the prolactin- releasing peptide (PRLH).
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Interleukin 10 receptor, beta subunit is a subunit for the interleukin-10 receptor. IL10RB is its human gene. IL10RB has also recently been designated CDW210B (cluster of differentiation W210B). The protein encoded by this gene belongs to the cytokine receptor family.
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Serine/threonine-protein kinase receptor R3 is an enzyme that in humans is encoded by the ACVRL1 gene. ACVRL1 is a receptor in the TGF beta signaling pathway. It is also known as activin receptor-like kinase 1, or ALK1.
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AMPARs are found in many parts of the brain and are the most commonly found receptor in the nervous system. The GRIA2-encoded AMPA receptor (see below) ligand binding core was the first glutamate receptor ion channel to be crystallized.
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The inhibitory glycine receptor mediates postsynaptic inhibition in the spinal cord and other regions of the central nervous system. It is a pentameric receptor composed of alpha and beta subunits. The GLRB gene encodes the beta subunit of the receptor.
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Antihistamines, which act on this receptor, are used as anti-allergy drugs. The crystal structure of the receptor has been determined (shown on the right) and used to discover new histamine H1 receptor ligands in structure-based virtual screening studies.
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The tyrosine kinase Lck functions either in conjunction with a co-receptor molecule (CD4 or CD8) or as a free Lck kinase. The kinetic-segregation model might be applied to both co-receptor dependent and co-receptor independent signaling through TCR.
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However, further studies in neutrophils indicated that 5-(S)-HETE acts through a receptor distinct from that used by LTB4 as well as various other neutrophil stimuli. This 5(S)-HETE receptor is termed the oxoeicosanoid receptor 1 (abbreviated as (OXER1).
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Chemokine like receptor 1 also known as ChemR23 ( _Chem_ erin _R_ eceptor _23_ ) is a protein that in humans is encoded by the CMKLR1 gene. Chemokine receptor-like 1 is a G protein-coupled receptor for the chemoattractant adipokine chemerin and the omega-3 fatty acid eicosapentaenoic acid-derived specialized pro-resolving molecule, resolvin E1 (see Specialized proresolving mediators#EPA-derived resolvins (i.e. RvE)). The murine receptor that shares almost 80% homology with the human receptor, is called Dez.
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Originally it was thought that the CB2 receptor was only expressed in peripheral tissue while the CB1 receptor is the endogenous receptor on neurons. Recent work with immunohistochemical staining has shown expression within neurons. Subsequently, it was shown that CB2 knock out mice, produced the same immunohistochemical staining, indicating the presence of the CB2 receptor where none was expressed. This has created a long history of debate as to the Central Nervous System expression of the CB2 receptor.
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Chemokine receptor CXCR3 is a Gαi protein-coupled receptor in the CXC chemokine receptor family. Other names for CXCR3 are G protein-coupled receptor 9 (GPR9) and CD183. There are three isoforms of CXCR3 in humans: CXCR3-A, CXCR3-B and chemokine receptor 3-alternative (CXCR3-alt). CXCR3-A binds to the CXC chemokines CXCL9 (MIG), CXCL10 (IP-10), and CXCL11 (I-TAC) whereas CXCR3-B can also bind to CXCL4 in addition to CXCL9, CXCL10, and CXCL11.
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The alpha-1A adrenergic receptor (α1A adrenoreceptor), also known as ADRA1A, formerly known also as the alpha-1C adrenergic receptor, is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it. There is no longer a subtype α1C receptor. At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. To avoid confusion, the naming convention was continued with the letter D.
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Type II receptor recruits type I receptor and phosphorylates The TGF beta ligand binds to a type II receptor dimer, which recruits a type I receptor dimer forming a hetero-tetrameric complex with the ligand. These receptors are serine/threonine kinase receptors. They have a cysteine rich extracellular domain, a transmembrane domain and a cytoplasmic serine/threonine rich domain. The GS domain of the type I receptor consists of a series of about thirty serine-glycine repeats.
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The DAF-1 gene encodes for a cell surface Enzyme-linked receptor of TGF-beta signaling pathway in the worm Caenorhabditis elegans. DAF-1 is one of the type I receptor of TGF-beta pathway. DAF-1 acts as a receptor protein serine/threonine kinase, is activated by type II receptor Daf-4 phosphorylation after the ligand Daf-7 binds to the receptor heterotetramer, and then phosphorylates Daf-8 or Daf-14, the SMAD proteins in C. elegans.
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This led to further research, resulting in the isolation of the genes that encoded the mammalian tachykinins and eventually the discovery of three different tachykinin receptors. In 1984, it was decided that the tachykinin receptors should be called tachykinin NK1 receptor, tachykinin NK2 receptor and tachykinin NK3 receptor. Biological research that identified the many functions of tachykinins sparked interest in neurokinin receptor antagonists development. In the 1980s, several peptide antagonists derived from SP were the first NK1 receptor antagonists.
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CGRP mediates its effects through a heteromeric receptor composed of a G protein-coupled receptor called calcitonin receptor-like receptor (CALCRL) and a receptor activity-modifying protein (RAMP1). CGRP receptors are found throughout the body, suggesting that the protein may modulate a variety of physiological functions in all major systems (e.g., respiratory, endocrine, gastrointestinal, immune, and cardiovascular). The extracellular loop number 2 is fundamental for ligand induced activation, with key interactions of R274/Y278/D280/W283.
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Arrestin binding to phosphorylated, active receptor prevents receptor stimulation of heterotrimeric G protein transducer proteins, blocking their cellular signaling and resulting in receptor desensitization. Arrestin binding also directs receptors to specific cellular internalization pathways, removing the receptors from the cell surface and also preventing additional activation. Arrestin binding to phosphorylated, active receptor also enables receptor signaling through arrestin partner proteins. Thus the GRK/arrestin system serves as a complex signaling switch for G protein-coupled receptors.
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IL-7 receptor and signaling, common γ chain (blue) and IL-7 receptor-α (green) The interleukin-7 receptor is a protein found on the surface of cells. It is made up of two different smaller protein chains - i.e. it is a heterodimer, and consists of two subunits, interleukin-7 receptor-α (CD127) and common-γ chain receptor (CD132). The common-γ chain receptors is shared with various cytokines, including interleukin-2, -4, -9, and -15.
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There are five types of kainate receptor subunits, GluR5 (), GluR6 (), GluR7 (), KA1 () and KA2 (), which are similar to AMPA and NMDA receptor subunits and can be arranged in different ways to form a tetramer, a four subunit receptor. GluR5-7 can form homomers (ex. a receptor composed entirely of GluR5) and heteromers (ex. a receptor composed of both GluR5 and GluR6), however, KA1 and KA2 can only form functional receptors by combining with one of the GluR5-7 subunits.
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Subsequently, other benzomorphans, such as pentazocine (an N-dimethylallylbenzomorphan), cyclazocine (an N-cyclopropylmethylbenzomorphan), and phenazocine (an N-phenylethylbenzomorphan), were developed, and some have been marketed for use as analgesics. The sigma σ1 receptor was named in 1976 and (+)-alazocine was described as its prototypical ligand. The receptor was initially thought to be an opioid receptor, and then was confused with the NMDA receptor for a time, but was ultimately distinguished from them both. The psychotomimetic effects of alazocine and the other benzomorphans were initially attributed incorrectly to agonism of the σ1 receptor; subsequent research established that the effects are in fact caused by agonism of the κ-opioid receptor and/or antagonism of the NMDA receptor.
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The existence of a specific GHB receptor was predicted by observing the action of GHB and related compounds that primarily act on the GABAB receptor, but also exhibit a range of effects which were found not to be produced by GABAB activity, and so were suspected of being produced by a novel and at the time unidentified receptor target. Following the discovery of the "orphan" G-protein coupled receptor GPR172A, it was subsequently found to be the GHB receptor whose existence had been previously predicted. The rat GHB receptor was first cloned and characterised in 2003 followed by the human receptor in 2007. Due to its many functions, this gene has a history of multiple discovery.
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The receptor for cysteinyl leukotrienes LTC4, LTD4 and LTE4 are a viable target because of the importance of cysteinyl leukotrienes in mediating the responses in asthma. It has been discovered that two types of said receptor exist, the CysLT1 receptor as well as the CysLT2 receptor. Leukotriene-receptor antagonists is a special class of drug, formulated as tablets that have both an anti-inflammatory effect as well as a bronchodilating effect. The development of leukotriene receptor antagonist started with screening a large number of compounds and designing quinoline and structural analogues. An example of a CysLT1 receptor antagonists is montelukast which is a quinoline derivative and zafirlukast which is an indole derivative.
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Angiotensin II receptor type 2, also known as the AT2 receptor is a protein that in humans is encoded by the AGTR2 gene.
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5-hydroxytryptamine (serotonin) receptor 1F, also known as HTR1F is a 5-HT1 receptor protein and also denotes the human gene encoding it.
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Both peptides, however, can act as full agonists on either receptor, although their potency is decreased when not bound to their specific receptor.
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While the TST detects NK1 receptor antagonists, which have known antidepressant action, it doesn't detect CRF1 receptor antagonists which also have antidepressant functions.
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ADBICA is a potent agonist of the CB1 receptor and CB2 receptor with an EC50 value of 0.69 nM and 1.8 nM respectively.
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Deficits in complement receptor expression can cause disease. Mutations in complement receptors which alter receptor function can also increase risk of certain diseases.
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NMDA receptor antagonists like ketamine and esketamine are rapid-acting antidepressants and seem to work via blockade of the ionotropic glutamate NMDA receptor.
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The aromatic bark contains magnolol, honokiol, 4-O-methylhonokiol, and obovatol. Magnolol and honokiol activate the nuclear receptor peroxisome proliferator-activated receptor gamma.
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As a partial agonist, buprenorphine binds and activates the opioid receptors, but has only partial efficacy at the receptor relative to a full agonist, even at maximal receptor occupancy. It is thus well-suited to treat opioid dependence, as it produces milder effects on the opioid receptor with lower dependence and abuse potential. Naloxone is a pure opioid antagonist that competes with opioid molecules in the CNS and prevents them from binding to the opioid receptors. Naloxone's binding affinity is highest for the μ-opioid receptor, then the δ-opioid receptor, and lowest for the κ-opioid receptor.
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The cannabinoid receptor type 2, abbreviated as CB2, is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the CNR2 gene. It is closely related to the cannabinoid receptor type 1, which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic- inhibition, the psychoactive properties of tetrahydrocannabinol, the active agent in cannabis, and other phytocannabinoids (plant cannabinoids). The principal endogenous ligand for the CB2 receptor is 2-Arachidonoylglycerol (2-AG). CB2 was cloned in 1993 by a research group from Cambridge looking for a second cannabinoid receptor that could explain the pharmacological properties of tetrahydrocannabinol.
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The protein receptor encoded by this gene is a member of the TNF-receptor superfamily. This receptor has been found to be essential in mediating a broad variety of immune and inflammatory responses including T cell-dependent immunoglobulin class switching, memory B cell development, and germinal center formation. AT-hook transcription factor AKNA is reported to coordinately regulate the expression of this receptor and its ligand, which may be important for homotypic cell interactions. The TNFR- receptor associated factor adaptor proteins TRAF1, TRAF2, TRAF6 and possibly TRAF5 interact with this receptor serve as mediators of the signal transduction.
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Additionally, ß-arrestins are better at inactivating ßARK-phosphorylated receptors rather than protein kinase A-phosphorylated receptors, which suggests that the arrestins preferentially mediate homologous desensitization. The mechanism of homologous desensitization for the β2 receptor is as follows: # Agonist binds and activates the receptor, which changes to an active conformational state. # Beta adrenergic receptor kinase (βARK), a cytoplasmic kinase is activated and phosphorylates the C-terminus of the β2 receptor. # This phosphorylation increases the affinity of β-arrestin for the receptor, resulting in uncoupling of the α subunit of the heterotrimeric G-protein from the receptor, producing desensitization.
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Ligands coated on the nanoparticle's surface bind to specific receptors to cause a conformational change. Once bound to these receptors, transcytosis can commence, and this involves the formation of vesicles from the plasma membrane pinching off the nanoparticle system after internalization. Additional receptors identified for receptor-mediated endocytosis of nanoparticle delivery systems are the scavenger receptor class B type I (SR-BI), LDL receptor (LRP1), transferrin receptor, and insulin receptor. As long as a receptor exists on the endothelial surface of the BBB, any ligand can be attached to the nanoparticle's surface to functionalize it so that it can bind and undergo endocytosis.
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LNK is widely expressed in human tissues, with the highest expression in hematopoietic cells. LNK negatively controls the activation of several receptors activation, including stem cell factor receptor (c-kit), thrombopoietin receptor (MPL), erythropoietin receptor (EPOR), platelet- derived growth factor receptor (PDGFR), macrophage colony-stimulating factor receptor (c-Fms), and their related pathways. LNK is a negative regulator of signaling in endothelial cells, such as the TNF signaling pathway, especially in inflammation. LNK has been found to function as a negative regulator in lymphopoiesis, megakaryopoiesis, erythropoiesis as well as HSC expansion by moderating growth factor and cytokine receptor-mediated signaling.
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Ligands that bind to RTKs include fibroblast growth factors, epidermal growth factors, platelet-derived growth factors, and stem cell factor. This dimerizes the transmembrane receptor to another RTK receptor, which causes the autophosphorylation and subsequent conformational change of the homodimerized receptor. This conformational change activates the dormant kinase of each RTK on the tyrosine residue. Due to the fact that the receptor spans across the membrane from the extracellular environment, through the lipid bilayer, and into the cytoplasm, the binding of the receptor to the ligand also causes the trans phosphorylation of the cytoplasmic domain of the receptor.
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MAGE-A11 is part of the androgen receptor signaling pathway in humans. It binds directly to the androgen receptor, promoting transcriptional through direct binding to the androgen receptor FXXLF motif region. This control is specific to primates, and is due to a mutation in the androgen receptor from alanine to valine at residue 33, which extends the α-helix, which enables direct MAGE-A11 binding to the androgen receptor. Post-translational modification of the protein by phosphorylation of Thr-360 and monoubiquitinylation of Lys-240 and Lys-245 also stabilizes the interaction with the androgen receptor.
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Adrenomedullin (AM) exerts its actions through combinations of the calcitonin receptor like receptor (CALCRL) or CLR; and either (Receptor activity-modifying protein) 2 (RAMP2) or RAMP3, (known as AM1 and AM2 receptors respectively). Both transduce the hormone binding to intracellular signaling via second messenger cascades. The AM2 receptor has a low affinity for CGRP, but this is of no physiological relevance. Unlike the classical one ligand-one receptor notion of receptor signalling, the interaction of both CALCRL and RAMP at the membrane is required for AM to mediate its action: neither can bind the hormone (and therefore transduce a signal) alone.
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For example, in GNRA-tetraloop interactions, the second nucleotide of the tetraloop stacks directly on an A-platform motif (see above) within the receptor. The sequence of the tetraloop and its receptor often covary so that the same type of tertiary contact can be made with different isoforms of the tetraloop and its cognate receptor. For example, the self- splicing group I intron relies on tetraloop receptor motifs for its structure and function. Specifically, the three adenine residues of the canonical GAAA motif stack on top of the receptor helix and form multiple stabilizing hydrogen bonds with the receptor.
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Pergolide acts as an agonist of dopamine D2 and D1 and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline. Although pergolide is more potent as an agonist of the D2 receptor, it has high D1 receptor affinity and is one of the most potent D1 receptor agonists of the dopamine receptor agonists that are clinically available. The agonist activity of pergolide at the D1 receptor somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease.
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Double positive thymocytes that have a T cell receptor capable of binding MHC class I or class II (even with a weak affinity) receive signalling through the T cell receptor. Thymocytes that have a T cell receptor incapable of binding MHC class I or class II undergo apoptosis. Some thymocytes are able to rescue failed positive selection by receptor editing (rearrangement of the other T cell receptor allele to produce a new T cell receptor). The double positive thymocytes undergo lineage commitment, maturing into a CD8+ T cell (recognising MHC class I) or a CD4+ T cell (recognising MHC class II).
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Studies using animals genetically engineered to lack EP3 and supplemented by studies examining the actions of EP3 receptor antagonists and agonists in animals as well as animal and human tissues indicate that this receptor serves various functions. However, an EP3 receptor function found in these studies does not necessarily indicate that in does do in humans. For example, EP3 receptor activation promotes duodenal secretion in mice; this function is mediated by EP4 receptor activation in humans. EP receptor functions can vary with species and most of the functional studies cited here have not translated their animal and tissue models to humans.
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After almost a century of receptor research, the adenosine A2A receptor has been selected as a possible research target for various medical conditions. Antagonists of the receptor have been researched, especially as an enhancer for the therapeutic effects of L-DOPA in Parkinson’s treatment. Certain evidence points to adenosine A2A receptor antagonism functioning in a neuroprotective manner in the brain. This effect has been noted for both non-selective and selective adenosine A2A receptor antagonists. This neuroprotective function is the manner in which A2A receptor antagonists might help to prevent diseases such as Alzheimer’s, Parkinson’s and Multiple sclerosis.
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SGA acts primarily as a high-affinity agonist of the progesterone receptor (272% of the affinity of progesterone and 136% of that of promegestone). It does not bind significantly to the androgen receptor, estrogen receptor, or mineralocorticoid receptor. As such, SGA does not have estrogenic, androgenic, antiandrogenic, or antimineralocorticoid activity. However, SGA does have significant affinity for the glucocorticoid receptor (38% of that of dexamethasone), but in spite of its relatively high affinity for the glucocorticoid receptor, it either does not have any glucocorticoid effects or shows glucocorticoid effects only at exceptionally high doses in animals.
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Naloxazone is an irreversible μ-opioid receptor antagonist which is selective for the μ1 receptor subtype. Naloxazone produces very long lasting antagonist effects as it forms a covalent bond to the active site of the mu-opioid receptor, thus making it impossible for the molecule to unbind and blocking the receptor permanently until the receptor is recycled by endocytosis. It has been reported that naloxazone is unstable in acidic solution, dimerizing into the more stable and much more potent antagonist naloxonazine. Under conditions in which no naloxonazine formation could be detected, naloxazone did not display irreversible μ opioid receptor binding.
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ACE-031 is an engineered decoy receptor used in attempts to treat children with Duchenne muscular dystrophy (DMD). The ACE-031 receptor circulates outside the muscle- fiber membrane. Because this receptor binds to myostatin, it lowers the amount of myostatin that can bind to the native receptor in the membrane (ActRIIB), preventing myostatin from delivering the muscle growth-limiting signal.
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IL-26 signals through a receptor complex comprising two distinct proteins called IL-20 receptor 1 and IL-10 receptor 2. By signaling through this receptor complex, IL-26 induces rapid phosphorylation of the transcription factors STAT1 and STAT3, which enhance IL-10 and IL-8 secretion and as expression of the CD54 molecule on the surface of epithelial cells.
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A proctolin receptor in Drosophila melanogaster has been recently identified as the orphan G-protein coupled receptor CG6986. The DNA of the gene sequence was cloned and expressed in mammalian cells and the expressed receptor was specific for proctolin. In Drosophila, this receptor is strongly expressed in the head, the larval hindgut, the aorta and on neuronal endings in adult hearts.
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If the membrane receptors are denatured or deficient, the signal transduction can be hindered and cause diseases. Some diseases are caused by disorders of membrane receptor function. This is due to deficiency or degradation of the receptor via changes in the genes that encode and regulate the receptor protein. The membrane receptor TM4SF5 influences the migration of hepatic cells and hepatoma.
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Etoxadrol is a non-competitive NMDA receptor antagonist. It binds with high affinity to the PCP binding site on the NMDA receptor (Ki = 107 nM, determined by the displacement of radiolabeled TCP). Normally, the inactivated NMDA receptor possesses a magnesium (Mg2+) block in the channel, blocking the passage of cations. NMDA receptor action in the absence (left) or presence (right) of etoxadrol.
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LP-12 is a drug which acts as a potent agonist at the 5HT7 serotonin receptor, with very high selectivity over other tested receptor subtypes such as the serotonin 5-HT1A and 5-HT2A, and the dopamine D2 receptor. It has been used to research the involvement of the 5-HT7 receptor in as yet poorly understood processes such as allodynia and hyperalgesia.
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In biochemistry, an orphan receptor is a protein that has a similar structure to other identified receptors but whose endogenous ligand has not yet been identified. If a ligand for an orphan receptor is later discovered, the receptor is referred to as an "adopted orphan". Conversely, the term orphan ligand refers to a biological ligand whose cognate receptor has not yet been identified.
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Mu and Kappa receptors are associated with aversion behaviors and Mu receptor density is greater in tethered sows than sows that are in groups outdoors. However, sows with stereotypy behaviors experienced a decrease both in Mu and Kappa receptor density in the brain suggesting that inactivity increases Mu receptor density and stereotypy development decrease both kappa and Mu receptor density.
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Interleukin 8 receptor, alpha is a chemokine receptor. This name and the corresponding gene symbol IL8RA have been replaced by the HGNC approved name C-X-C motif chemokine receptor 1 and the approved symbol CXCR1. It has also been designated as CD181 (cluster of differentiation 181). The IUPHAR Committee on Receptor Nomenclature and Drug Classification use the HGNC recommended name, CXCR1.
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Gonadotropin-releasing hormone receptor is a protein that in humans is encoded by the GNRHR gene. This gene encodes the receptor for type 1 gonadotropin- releasing hormone. This receptor is a member of the seven-transmembrane, G-protein coupled receptor (GPCR) family. It is expressed on the surface of pituitary gonadotrope cells as well as lymphocytes, breast, ovary, and prostate.
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BD1067 or N-[2-(3,4-dichlorophenyl)ethyl]-N-ethyl-1-pyrrolidineethanamine is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 2 ± 0.5 nM for the sigma-1 receptor and greater than 19 times selectivity over the sigma-2 receptor. Like other sigma receptor antagonists, pretreating Swiss Webster mice with BD1067 significantly attenuates the behavioral toxicity of cocaine.
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It is also known to be an entry co-receptor for HIV-1. This gene and seven other chemokine receptor genes form a chemokine receptor gene cluster on the chromosomal region 3p21. Alternatively spliced transcript variants encoding the same protein have been described.
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Short transient receptor potential channel 5 (TrpC5) also known as transient receptor protein 5 (TRP-5) is a protein that in humans is encoded by the TRPC5 gene. TrpC5 is subtype of the TRPC family of mammalian transient receptor potential ion channels.
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Within B and T cells, respectively, Syk and Zap-70 transmit signals from the B-Cell receptor and T-Cell receptor. Syk plays a similar role in transmitting signals from a variety of cell surface receptors including CD74, Fc Receptor, and integrins.
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Interleukin-10 receptor is a type II cytokine receptor. The receptor is tetrameric, composed of 2α and 2β subunits. The α subunit is expressed on haematopoietic cells (such as T, B, NK, mast, and dendritic cells) whilst the β subunit is expressed ubiquitously.
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BIK1 is a receptor-like cytoplasmic kinase (RLCK) that associates with a cell-surface receptor, FLS2, and a co- receptor kinase, BAK1 to transduce signals when a PAMP is detected. In order for BIK1 to be activated, site-specific phosphorylation must occur.
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Masitinib inhibits the receptor tyrosine kinase c-Kit which is displayed by various types of tumour. It also inhibits the platelet derived growth factor receptor (PDGFR), lymphocyte-specific protein tyrosine kinase (Lck), focal adhesion kinase (FAK) and fibroblast growth factor receptor 3 (FGFR3).
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Dopamine receptor mutations can cause genetic hypertension in humans. This can occur in animal models and humans with defective dopamine receptor activity, particularly D1.
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Membrane progesterone receptor beta (mPRβ), or progestin and adipoQ receptor 8 (PAQR8), is a protein that in humans is encoded by the PAQR8 gene.
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Vasoactive intestinal peptide receptor 2 also known as VPAC2, is a G-protein coupled receptor that in humans is encoded by the VIPR2 gene.
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GDNF family receptor alpha-2 (GFRα2), also known as the neurturin receptor, is a protein that in humans is encoded by the GFRA2 gene.
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This causes the recruitment of a BMP type I receptor, which it phosphorylates. The Type I receptor phosphorylates an R-SMAD a transcriptional regulator.
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Dantrolene depresses excitation-contraction coupling in skeletal muscle by acting as a receptor antagonist to the ryanodine receptor, and decreasing free intracellular calcium concentration.
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The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the human gene encoding it.
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GDNF family receptor alpha-3 (GFRα3), also known as the artemin receptor, is a protein that in humans is encoded by the GFRA3 gene.
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Interleukin-22 receptor is a type II cytokine receptor. It binds to Interleukin-22. It is a heterodimer of α1 and IL-10Rβ2 subunits.
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Iodoresiniferatoxin (I-RTX) is a strong competitive antagonist of the Transient Receptor Potential Vanilloid 1 (TRPV1) receptor. I-RTX is derived from resiniferatoxin (RTX).
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The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the human gene encoding it.
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Membrane progesterone receptor epsilon (mPRɛ), or progestin and adipoQ receptor 9 (PAQR9), is a protein that in humans is encoded by the PAQR9 gene.
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Pancreatic polypeptide receptor 1, also known as Neuropeptide Y receptor type 4, is a protein that in humans is encoded by the PPYR1 gene.
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Membrane progesterone receptor gamma (mPRγ), or progestin and adipoQ receptor 5 (PAQR5), is a protein that in humans is encoded by the PAQR5 gene.
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Membrane progesterone receptor delta (mPRδ), or progestin and adipoQ receptor 6 (PAQR6), is a protein that in humans is encoded by the PAQR6 gene.
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GDNF family receptor alpha-1 (GFRα1), also known as the GDNF receptor, is a protein that in humans is encoded by the GFRA1 gene.
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MED14 has been shown to interact with PPARGC1A, Estrogen receptor alpha, STAT2, Cyclin-dependent kinase 8, Glucocorticoid receptor and Hepatocyte nuclear factor 4 alpha.
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ET-2 acts by binding to two different G-protein coupled receptors (GCPRs), the endothelin A receptor (EDNRA) and the endothelin B receptor (EDNRB).
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Membrane progesterone receptor alpha (mPRα), or progestin and adipoQ receptor 7 (PAQR7), is a protein that in humans is encoded by the PAQR7 gene.
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Binding at the α1β3γ2 GABAA receptor. Alprazolam with red space-filling carbon atoms. γ2 receptor subunit in mint green. The α1' subunit is hidden.
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They are called receptors because when these come into contact with particular molecules (termed ligands), then chemical changes are induced to the receptor. These changes typically involve alterations in the three-dimensional shape of the receptor. These 3D structure changes affect both the extracellular and intracellular parts (domains) of the receptor. As a result, interaction of a receptor with its specific ligand which is located outside of the cell causes changes to the receptor part which is inside the cell.
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The main problem with the development of NMDA antagonists for neuroprotection is that physiological NMDA receptor activity is essential for normal neuronal function. Complete blockade of all NMDA receptor activity results in side effects such as hallucinations, agitation and anesthesia. To be clinically relevant, an NMDA receptor antagonist must limit its action to blockade of excessive activation, without limiting normal function of the receptor. Figure 3 shows simplified models of various types of NMDA receptor antagonists, which will be discussed further.
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Interleukin-2 receptor alpha chain (also called CD25) is a protein that in humans is encoded by the IL2RA gene. The interleukin 2 (IL2) receptor alpha (IL2RA) and beta (IL2RB) chains, together with the common gamma chain (IL2RG), constitute the high-affinity IL2 receptor. Homodimeric alpha chains (IL2RA) result in low-affinity receptor, while homodimeric beta (IL2RB) chains produce a medium-affinity receptor. Normally an integral-membrane protein, soluble IL2RA has been isolated and determined to result from extracellular proteolysis.
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Oxoeicosanoid receptor 1 (OXER1) also known as G-protein coupled receptor 170 (GPR170) is a protein that in humans is encoded by the OXER1 gene located on human chromosome 2p21; it is the principle receptor for the 5-Hydroxyicosatetraenoic acid family of carboxy fatty acid metabolites derived from arachidonic acid. The receptor has also been termed hGPCR48, HGPCR48, and R527 but OXER1 is now its preferred designation. OXER1 is a G protein-coupled receptor (GPCR) that is structurally related to the hydroxy-carboxylic acid (HCA) family of G protein-coupled receptors whose three members are HCA1 (GPR81), HCA2 (Niacin receptor 1), and HCA3 (Niacin receptor 2); OXER1 has 30.3%, 30.7%, and 30.7% amino acid sequence identity with these GPCRs, respectively. It is also related (30.4% amino acid sequence identity) to the recently defined receptor, GPR31, for the hydroxyl-carboxy fatty acid 12-HETE.
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In enzymology, a low-density-lipoprotein receptor kinase () is an enzyme that catalyzes the chemical reaction :ATP + [low-density-lipoprotein receptor]-L-serine \rightleftharpoons ADP + [low-density-lipoprotein receptor]-O-phospho-L-serine Thus, the two substrates of this enzyme are ATP and low-density-lipoprotein receptor]-L-serine, whereas its two products are ADP and low-density-lipoprotein receptor]-O-phospho-L-serine. This enzyme belongs to the family of transferases, specifically those transferring a phosphate group to the sidechain oxygen atom of serine or threonine residues in proteins (protein-serine/threonine kinases). The systematic name of this enzyme class is ATP:[low-density-lipoprotein receptor]-L-serine O-phosphotransferase. Other names in common use include ATP:low-density- lipoprotein-L-serine O-phosphotransferase, LDL receptor kinase, [low-density- lipoprotein] kinase, low-density lipoprotein kinase, low-density-lipoprotein receptor kinase (phosphorylating), and STK7.
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Barbiturates produce their pharmacological effects by increasing the duration of chloride ion channel opening at the GABAA receptor (pharmacodynamics: This increases the efficacy of GABA), whereas benzodiazepines increase the frequency of the chloride ion channel opening at the GABAA receptor (pharmacodynamics: This increases the potency of GABA). The direct gating or opening of the chloride ion channel is the reason for the increased toxicity of barbiturates compared to benzodiazepines in overdose. Further, barbiturates are relatively non-selective compounds that bind to an entire superfamily of ligand-gated ion channels, of which the GABAA receptor channel is only one of several representatives. This Cys-loop receptor superfamily of ion channels includes the neuronal nACh receptor channel, the 5-HT3 receptor channel, and the glycine receptor channel.
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The cytoplasmic tail of the mannose receptor does not contain any signalling motifs, yet the receptor has proven to be essential for production of both pro- and anti-inflammatory cytokines, indicating a more passive role for the receptor in phagocytosis of pathogens. This suggests that the mannose receptor is assisted by other cell surface receptors in order to trigger a signalling cascade. For example, it has been shown that HEK 293 cells co-transfected with human mannose receptor and human Toll-like receptor 2 cDNA are able to secrete IL-8 in response to P. carinii infection, whereas those transfected with either receptor alone did not. It is possible that the two receptors form a complex on the cell surface that facilitates signal transduction upon pathogenic challenge.
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Celiprolol is a medication in the class of beta blockers, used in the treatment of high blood pressure. It has a unique pharmacology: it is a selective β1 receptor antagonist, but a β2 receptor partial agonist. It is also a weak α2 receptor antagonist.
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G-protein coupled receptor 31 also known as 12-(S)-HETE receptor is a protein that in humans is encoded by the GPR31 gene. The human gene is located on chromosome 6q27 and encodes a G-protein coupled receptor protein composed of 319 amino acids.
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5-Hydroxytryptamine receptor 2B (5-HT2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the HTR2B gene. 5-HT2B is a member of the 5-HT2 receptor family that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT).
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Repeated administration of receptor agonists may result in receptor internalization and/or a reduction in receptor protein signalling. The inverse agonist MK-9470 makes it possible to produce in vivo images of the distribution of CB1 receptors in the human brain with positron emission tomography.
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It has also been used to mask σ1 receptor sites so that σ2 receptor binding characteristics in the rat liver could be determined, by labeling σ2 receptor sites with [3H]l,3-di-o-tolylguanidine (DTG) in the presence of 1 μM dextrallorphan solution.
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Human urotensin II receptor is located on chromosome 17q25 as an intronless gene. There are no known subtypes of the receptor but the possibility cannot be discounted. It has similar domain sequences to the somatostatin receptor, and in lab conditions can be activated by somatostatin.
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The gene for the LHCGR is found on chromosome 2 p21 in humans, close to the FSH receptor gene. It consists of 70 kbp (versus 54 kpb for the FSHR). The gene is similar to the gene for the FSH receptor and the TSH receptor.
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Stress can also result in inheritable changes DNA methylation in the promoter regions of the estrogen receptor alpha (ERα), glucocorticoid receptor (GR), and mineralocorticoid receptor (MR). These changes lead to altered expression of these genes in offspring that in turn leads to decreased stress tolerance.
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AIP has been shown to interact with the aryl hydrocarbon receptor, peroxisome proliferator-activated receptor alpha and the aryl hydrocarbon receptor nuclear translocator. Further, it has shown that AIP can interact with IRF7 to exert its novel function of negatively regulating antiviral signal pathways.
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The photoreceptor cell-specific nuclear receptor (PNR), also known as NR2E3 (nuclear receptor subfamily 2, group E, member 3), is a protein that in humans is encoded by the NR2E3 gene. PNR is a member of the nuclear receptor super family of intracellular transcription factors.
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Relaxin/insulin-like family peptide receptor 1, also known as RXFP1, is a human G protein coupled receptor that is one of the relaxin receptors.
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Motilin receptor is a G protein-coupled receptor that binds motilin. Motilin in turn is an intestinal peptide that stimulates contraction of gut smooth muscle.
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The alpha-1B adrenergic receptor (α1B adrenoreceptor), also known as ADRA1B, is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it.
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The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it.
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The alpha-2C adrenergic receptor (α2C adrenoceptor), also known as ADRA2C, is an alpha-2 adrenergic receptor, and also denotes the human gene encoding it.
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Transmembrane interactions between TMEM59 and the wnt receptor Frizzled were found to drive receptor multimerization that leads to improved potency and efficiacy of wnt signaling.
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Interleukin 1 receptor, type II (IL-1R2) also known as CD121b (Cluster of Differentiation 121b) is an interleukin receptor. IL1R2 also denotes its human gene.
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Glutamate ionotropic receptor AMPA type subunit 2 (ionotropic glutamate receptor 2) is a protein that in humans is encoded by the GRIA2 (or GLUR2) gene.
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This receptor functionally interacts with toll-like receptor 2 (TLR2) to mediate cellular response to gram-positive bacteria, mycoplasma, fungi, some viruses and even protozoa.
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In 2007, it was well established that serotype I did not work with the FCoV fAPN receptor. The FCoV type I receptor still is unknown.
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LY255283 has been presented as a "selective" BLT2 receptor antagonist. However, this compound is also a BLT1 receptor agonists and therefore cannot be used to discriminate between these two receptor types. In all of the studies using LY255283 quoted above, other methods, such as siRNA knockdown, were used in conjunction with LY255283 to identify BLT2-dependency. Currently, there are no reports on selective BLT2 receptor antagonists.
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GPR113 Var 1 contains 1079 Amino Acids, and is integral to the plasma membrane. The 7-pass receptor contains 4 domains highlighted in the figure at right: Signal Peptide (Red), Hormone Receptor Domain (Blue), Latrophilin/CL-1-like GPS domain (Orange), and the 7-transmembrane receptor (Purple). Between the Hormone Receptor Domain and the GPS is a Domain of unknown function that is not highlighted.
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GPR156 (G protein-coupled receptor 156), is a human gene which encodes a G protein-coupled receptor belonging to metabotropic glutamate receptor subfamily. By sequence homology, this gene was proposed as being a possible GABAB receptor subunit, however when expressed in cells alone or with other GABAB subunits, no response to GABAB ligands could be detected. Therefore, the function of this protein remains to be elucidated.
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The protein encoded by this gene is a member of the TNF-receptor superfamily. This receptor is especially abundant in hematologic tissues. It has been shown to activate the NF-kappaB pathway and selectively bind TNF receptor-associated factor 1 (TRAF1). This receptor is capable of stimulating T-cell proliferation in the presence of CD3 signaling, which suggests its regulatory role in immune response.
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Soluble transferrin receptor conventionally refers to the cleaved extracellular portion of transferrin receptor 1 that is released into serum. This receptor is a protein dimer of two identical subunits, linked together by two pairs of disulfide bonds. Its molecular mass 190,000 Dalton. Blood testing of the soluble transferrin receptor (sTfR) is used as a measure of functional iron status and the investigation of iron deficiency anemia.
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This gene encodes a receptor for the OX-2 membrane glycoprotein. Both the receptor and substrate are cell surface glycoproteins containing two immunoglobulin-like domains. This receptor is restricted to the surfaces of myeloid lineage cells and the receptor-substrate interaction may function as a myeloid downregulatory signal. Mouse studies of a related gene suggest that this interaction may control myeloid function in a tissue-specific manner.
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Interleukin-17 receptor B is a protein that in humans is encoded by the IL17RB gene. The protein encoded by this gene is a cytokine receptor. This receptor specifically binds to IL17B and IL17E (IL25), but does not bind to IL17(A) or IL17C. This receptor has been shown to mediate the activation of NF-κB and the production of IL8 induced by IL17E.
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NGF binds with at least two classes of receptors: the tropomyosin receptor kinase A (TrkA) and low- affinity NGF receptor (LNGFR/p75NTR). Both are associated with neurodegenerative disorders. When NGF binds to the TrkA receptor, it drives the homodimerization of the receptor, which in turn causes the autophosphorylation of the tyrosine kinase segment. This leads to the activation of PI 3-kinase, ras, and PLC signaling pathways.
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Receptor-linked tyrosine kinases such as the epidermal growth factor receptor (EGFR) are activated by extracellular ligands, such as epidermal growth factor (EGF). Binding of EGF to the EGFR activates the tyrosine kinase activity of the cytoplasmic domain of the receptor. The EGFR becomes phosphorylated on tyrosine residues. Docking proteins such as GRB2 contain an SH2 domain that binds to the phosphotyrosine residues of the activated receptor.
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The peptide is less effective (IC50 ≈3 μM) at α7 nicotinic acetylcholine receptors. The peptide displayed low affinity to α4β2 and α3-containing muscle nicotinic acetylcholine receptor. The peptide showed no effect on the GABA receptor and the 5-HT receptor at concentrations up to respectively 100 μm and 10 μm. In conclusion, azemiopsin shows high selectivity in inhibiting certain nicotinic acetylcholine receptor subtypes.
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FGFR1OP2, when fused with the fibroblast growth factor receptor 1 (FGFR1), is shown to cause myeloproliferative syndrome. The protein encoded by the FGFR1 gene belongs to the fibroblast growth factor receptor family. FGFRs usually contain an extracellular ligand binding domain, a single transmembrane domain, and an intracellular tyrosine kinase domain. The extracellular domain specifies which ligand the receptor will bind to and mediates ligand-induced receptor dimerization.
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In the third intracellular loop of the receptor a protein kinase A and protein kinase c phosphorylation motifs have been detected. ACTH receptors also require the binding of melanocortin-2 receptor accessory protein-1 (MRAP1) without which ACTH receptors cannot bind ACTH. Without MRAP, the receptor is degraded in the endoplasmic reticulum, but with MRAP, the receptor is glycosylated and expressed on the cell plasma membrane.
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The KiSS1-derived peptide receptor (also known as GPR54 or the Kisspeptin receptor) is a G protein-coupled receptor which binds the peptide hormone kisspeptin (metastin). Kisspeptin is encoded by the metastasis suppressor gene KISS1, which is expressed in a variety of endocrine and gonadal tissues. Activation of the kisspeptin receptor is linked to the phospholipase C and inositol trisphosphate second messenger cascades inside the cell.
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The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R). It belongs to the tachykinin receptor sub-family of GPCRs. Other neurokinin subtypes and neurokinin receptors that interact with SP have been reported as well. Amino acid residues that are responsible for the binding of SP and its antagonists are present in the extracellular loops and transmembrane regions of NK-1.
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IGFBP-3 enters the cell nucleus by a mechanism that is incompletely understood, but involves its binding to importin-β. Within the nucleus, it can modulate nuclear hormone receptor activity by direct binding to retinoid X receptor, retinoic acid receptor, vitamin D receptor, PPARγ, and nur77, IGFBP-3 also interacts with DNA-dependent protein kinase within the nucleus to promote the repair of DNA damage.
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Studies using animals genetically engineered to lack EP4 and supplemented by studies examining the actions of EP4 receptor antagonists and agonists in animals as well as animal and human tissues indicate that this receptor serves various functions. However, an EP4 receptor function found in these studies does not necessarily indicate that in does so in humans since EP receptor functions can vary between species.
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5-hydroxytryptamine receptor 3A is a protein that in humans is encoded by the HTR3A gene. The product of this gene belongs to the ligand-gated ion channel receptor superfamily. This gene encodes subunit A of the type 3 receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor causes fast, depolarizing responses in neurons after activation.
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Endothelial protein C receptor (EPCR) also known as activated protein C receptor (APC receptor) is a protein that in humans is encoded by the PROCR gene. PROCR has also recently been designated CD201 (cluster of differentiation 201). The protein encoded by this gene is a receptor for protein C that enhances its activation. Protein C is an anti-coagulant serine protease activated by the blood coagulation pathway.
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Some work has shown that anandamide can bind to the vannilloid receptor VR1, the receptor responsible for mediating the effects of capsaicin. This receptor is present in the brain, and anandamide actions at this receptor may potentially contribute to DSE (Cristino et al. 2006, Hajos et al. 2002). However DSE is currently a largely unexplored phenomenon and more research is needed to draw any firm conclusions.
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Relaxin interacts with the relaxin receptor LGR7 (RXFP1) and LGR8 (RXFP2), which belong to the G protein-coupled receptor superfamily. They contain a heptahelical transmembrane domain and a large glycosylated ectodomain, distantly related to the receptors for the glycoproteohormones, such as the LH-receptor or FSH-receptor. Relaxin receptors have been found in the heart, smooth muscle, the connective tissue, and central and autonomous nervous system.
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Janus kinase 2 (commonly called JAK2) is a non-receptor tyrosine kinase. It is a member of the Janus kinase family and has been implicated in signaling by members of the type II cytokine receptor family (e.g. interferon receptors), the GM-CSF receptor family (IL-3R, IL-5R and GM-CSF-R), the gp130 receptor family (e.g., IL-6R), and the single chain receptors (e.g.
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Insulin receptor substrate 4 is a protein that in humans is encoded by the IRS4 gene. IRS4 encodes the insulin receptor substrate 4, a cytoplasmic protein that contains many potential tyrosine and serine/threonine phosphorylation sites. Tyrosine-phosphorylated IRS4 protein has been shown to associate with cytoplasmic signalling molecules that contain SH2 domains. The IRS4 protein is phosphorylated by the insulin receptor tyrosine kinase upon receptor stimulation.
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Interleukin 11 receptor, alpha subunit is a subunit of the interleukin 11 receptor. IL11RA is its human gene. Interleukin 11 is a stromal cell-derived cytokine that belongs to a family of pleiotropic and redundant cytokines that use the gp130 transducing subunit in their high affinity receptors. This gene encodes the IL-11 receptor, which is a member of the hematopoietic cytokine receptor family.
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LR132 or (+)-3,4-dichloro-N-[(1R,2S)-2-(1-pyrrolidinyl)cyclohexyl]benzeneethanamine is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 2 ± 0.1 nM for the sigma-1 receptor and more than 350 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with LR132 significantly decreases the convulsivity and lethality of cocaine.
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BD1052 or N-[2-(3,4-dichlorophenyl)ethyl]-N-2-propen-1-yl-1-pyrrolidineethanamine is a selective sigma receptor agonist, with a reported binding affinity of Ki = 2 ± 0.5 nM for the sigma-1 receptor and 30 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor agonists, pretreating Swiss Webster mice with BD1052 significantly increases the behavioral toxicity of cocaine.
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Toll-like receptor 6 is a protein that in humans is encoded by the TLR6 gene. TLR6 is a transmembrane protein, member of toll-like receptor family, which belongs to the pattern recognition receptor (PRR) family. TLR6 acts in a heterodimer form with toll-like receptor 2 (TLR2). Its ligands include multiple diacyl lipopeptides derived from gram-positive bacteria and mycoplasma and several fungal cell wall saccharides.
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As an SPRM, ulipristal acetate has partial agonistic as well as antagonistic effects on the progesterone receptor. Ulipristal acetate exhibits similar potency to antagonize progesterone receptor as mifepristone in vitro. It also binds to the androgen receptor and the glucocorticoid receptor, but is only a weak antiandrogen and antiglucocorticoid relative to flutamide and mifepristone, respectively. Ulipristal acetate has no relevant affinity to the estrogen and mineralocorticoid receptors.
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A CXCR4 antagonist is a substance which blocks the CXCR4 receptor and prevent its activation. Blocking the receptor stops the receptor's ligand, CXCL12, from binding which prevents downstream effects. CXCR4 antagonists are especially important for hindering cancer progression because one of the downstream effects initiated by CXCR4 receptor activation is cell movement which helps the spread of cancer, known as metastasis. The CXCR4 receptor has been targeted by antagonistic substances since being identified as a co- receptor in HIV and assisting the development of cancer.
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Androgen receptor The mechanism behind SBMA is caused by expansion of a CAG repeat in the first exon of the androgen receptor gene (trinucleotide repeats). The CAG repeat encodes a polyglutamine tract in the androgen receptor protein. The greater the expansion of the CAG repeat, the earlier the disease onset and more severe the disease manifestations. The repeat expansion likely causes a toxic gain of function in the receptor protein, since loss of receptor function in androgen insensitivity syndrome does not cause motor neuron degeneration.
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The Thornton lab has also been able to show that evolution is irreversible studying the glucocorticoid receptor. This receptor was changed by seven mutations in a cortisol receptor, but reversing these mutations didn't give the original receptor back. Indicating that epistasis plays a major role in protein evolution – an observation that in combination with the observations of several examples of parallel evolution, support the neutral network model mentioned above. Other earlier neutral mutations acted as a ratchet and made the changes to the receptor irreversible.
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The sigma-2 receptor (σ2R) is a sigma receptor subtype that has attracted attention due to its involvement in diseases such as cancer and neurological diseases. It is currently under investigation for its potential diagnostic and therapeutic uses. Although the sigma-2 receptor was identified as a separate pharmacological entity from the sigma-1 receptor in 1990, the gene that codes for the receptor was identified as TMEM97 only in 2016. TMEM97 was shown to regulate the cholesterol transporter NPC1 and to be involved in cholesterol homeostasis.
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This gene encodes the insulin receptor substrate 2, a cytoplasmic signaling molecule that mediates effects of insulin, insulin- like growth factor 1, and other cytokines by acting as a molecular adaptor between diverse receptor tyrosine kinases and downstream effectors. The product of this gene is phosphorylated by the insulin receptor tyrosine kinase upon receptor stimulation, as well as by an interleukin 4 receptor-associated kinase in response to IL4 treatment. Mice lacking IRS2 have a diabetic phenotype as well as a 40% reduction in brain mass.
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Low density lipoprotein receptor-related protein 1 (LRP1), also known as alpha-2-macroglobulin receptor (A2MR), apolipoprotein E receptor (APOER) or cluster of differentiation 91 (CD91), is a protein forming a receptor found in the plasma membrane of cells involved in receptor-mediated endocytosis. In humans, the LRP1 protein is encoded by the LRP1 gene. LRP1 is also a key signalling protein and, thus, involved in various biological processes, such as lipoprotein metabolism and cell motility, and diseases, such as neurodegenerative diseases, atherosclerosis, and cancer.
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The decision of which pathway is activated most likely depends on which Wnt ligand and Fz receptor are present, as well as the cellular context. Nineteen Wnt ligands and ten different members of the Fz seven-transmembrane receptor family have been described in the human genome. As a result, a large variety of responses could be initiated from the Wnt/Fz interactions. The Wnt/β-catenin pathway starts with the binding of Wnt to a receptor complex encompassing a Fz receptor and LRP co-receptor.
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When a bone morphogenetic protein binds to a receptor (BMP type 1 receptor kinase) it causes SMAD9 to interact with SMAD anchor for receptor activation (SARA).The binding of ligands causes the phosphorylation of the SMAD9 protein and the dissociation from SARA and the association with SMAD4. It is subsequently transferred to the nucleus where it forms complexes with other proteins and acts as a transcription factor. SMAD9 is a receptor regulated SMAD (R-SMAD) and is activated by bone morphogenetic protein type 1 receptor kinase.
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Chimeric antigen receptor T cell immunotherapy (CAR-T), possibly combined with cytokines and checkpoint inhibitors, are a regularly used form of immune gene therapy. CAR-T involves manipulation of a patient's natural T cells to express a chimeric antigen receptor. This receptor, now on millions of the patient's T cells, recognizes cancerous cells that express specific antigens. Usually, the T cell antigen receptor is inactive but when the receptor recognizes a certain cancerous antigen, the physical structure of the T cell changes to destroy the cancer cell.
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Growth factor receptor-bound protein 14 is a protein that in humans is encoded by the GRB14 gene. The product of this gene belongs to a small family of adapter proteins that are known to interact with a number of receptor tyrosine kinases and signaling molecules. This gene encodes a growth factor receptor- binding protein that interacts with insulin receptors and insulin-like growth- factor receptors. This protein likely has an inhibitory effect on receptor tyrosine kinase signaling and, in particular, on insulin receptor signaling.
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A "tyrosine kinase" is an enzyme which is capable of adding a phosphate group to the certain tyrosines on target proteins, or "substrates". A receptor tyrosine kinase is a "tyrosine kinase" which is located at the cellular membrane, and is activated by binding of a ligand via its extracellular domain. Other example of tyrosine kinase receptors include the insulin receptor, the IGF-1 receptor, the MuSK protein receptor, the vascular endothelial growth factor (VEGF) receptor, etc. The "substrate" proteins which are phosphorylated by TrkC include PI3 kinase.
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Bile acids also act as steroid hormones, secreted from the liver, absorbed from the intestine and having various direct metabolic actions in the body through the nuclear receptor Farnesoid X receptor (FXR), also known by its gene name . Another bile acid receptor is the cell membrane receptor known as G protein-coupled bile acid receptor 1 or TGR5. Many of their functions as signaling molecules in the liver and the intestines are by activating FXR, whereas TGR5 may be involved in metabolic, endocrine and neurological functions.
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Fig.1 A simple illustration of how two acetylcholine molecules bind to its receptive sites on the nicotinic receptorQuaternary muscle relaxants bind to the nicotinic acetylcholine receptor and inhibit or interfere with the binding and effect of ACh to the receptor. Each ACh-receptor has two receptive sites and activation of the receptor requires binding to both of them. Each receptor site is located at one of the two α-subunits of the receptor. Each receptive site has two subsites, an anionic site that binds to the cationic ammonium head and a site that binds to the blocking agent by donating a hydrogen bond.
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The CB2 receptor is encoded by the CNR2 gene. Approximately 360 amino acids comprise the human CB2 receptor, making it somewhat shorter than the 473-amino-acid-long CB1 receptor. As is commonly seen in G protein-coupled receptors, the CB2 receptor has seven transmembrane spanning domains, a glycosylated N-terminus, and an intracellular C-terminus. The C-terminus of CB2 receptors appears to play a critical role in the regulation of ligand-induced receptor desensitization and downregulation following repeated agonist application, perhaps causing the receptor to become less responsive to particular ligands. The human CB1 and the CB2 receptors possess approximately 44% amino acid similarity.
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Setipiprant binds to the DP2 receptor with a dissociation constant of 6 nM, representing potent antagonism of the receptor. The DP2 receptor, also called the CRTh2 receptor, is a G-protein-coupled receptor (GPCR) that is expressed on certain inflammatory cells, such as eosinophils, basophils, and certain lymphocytes. For its mechanism of action in the treatment of allergic conditions, setipiprant's DP2 antagonism prevents the action of prostaglandin D2 (PGD2) on these receptors. The DP2 receptor mediates the activation of type 2 helper T (Th2) cells, eosinophils, and basophils in the lungs, which are white blood cells implicated in producing the inflammatory response the characterizes allergic conditions.
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The melanocortin 1 receptor (MC1R), also known as melanocyte-stimulating hormone receptor (MSHR), melanin-activating peptide receptor, or melanotropin receptor, is a G protein–coupled receptor that binds to a class of pituitary peptide hormones known as the melanocortins, which include adrenocorticotropic hormone (ACTH) and the different forms of melanocyte-stimulating hormone (MSH). It is coupled to Gαs and upregulates levels of cAMP by activating adenylyl cyclase in cells expressing this receptor. It is normally expressed in skin and melanocytes, and to a lesser degree in periaqueductal gray matter, astrocytes and leukocytes. In skin cancer, M1CR is highly expressed in melanomas but not carcinomas.
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Selective glucocorticoid receptor modulators (SEGRMs) and selective glucocorticoid receptor agonists (SEGRAs) formerly known as dissociated glucocorticoid receptor agonists (DIGRAs) are a class of experimental drugs designed to share many of the desirable anti-inflammatory, immunosuppressive, or anticancer properties of classical glucocorticoid drugs but with fewer side effects such as skin atrophy. Although preclinical evidence on SEGRAMs’ anti- inflammatory effects are culminating, currently, the efficacy of these SEGRAMs on cancer are largely unknown. Selective glucocorticoid receptor agonists (SEGRAs) are historically and typically steroidal in structure while selective glucocorticoid receptor modulators (SEGRMs) are typically nonsteroidal. The combined abbreviation of selective glucocorticoid receptor agonist and modulator is SEGRAM.
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Specifically, Block et al. report that the human musk-recognizing receptor, OR5AN1, identified using a heterologous olfactory receptor expression system and robustly responding to cyclopentadecanone and muscone, fails to distinguish isotopomers of these compounds in vitro. Furthermore, the mouse (methylthio)methanethiol-recognizing receptor, MOR244-3, as well as other selected human and mouse olfactory receptors, responded similarly to normal, deuterated, and carbon-13 isotopomers of their respective ligands, paralleling results found with the musk receptor OR5AN1. Based on these findings, the authors conclude that the proposed vibration theory does not apply to the human musk receptor OR5AN1, mouse thiol receptor MOR244-3, or other olfactory receptors examined.
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At least four different GPCR-linked proteins are known to respond to steroid hormones. G Protein-Coupled Receptor 30 (GPR30) binds estrogen, Membrane Progestin Receptor (mPR) binds progesterone, G Protein-Coupled Receptor Family C Group 6 Member A (GPRC6A) binds androgens, and Thyroid Hormone and Trace Amine Associated Receptor 1 (TAAR1) binds Thyroid hormone (though not technically steroid hormones, thyroid hormones can be grouped here because their receptors belong to the nuclear receptor superfamily). As an example of the effects of these GPCR- linked proteins consider GPR30. GPR30 binds estrogen, and upon binding estrogen this pathway activates adenylyl cyclase and epidermal growth factor receptor.
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The activity of the NMDA receptor is affected by many psychoactive drugs such as phencyclidine (PCP), alcohol (ethanol) and dextromethorphan (DXM). The anaesthetic and analgesic effects of the drugs ketamine and nitrous oxide are partially due to their effects on NMDA receptor activity. Since 1989 memantine has been recognized to be an uncompetitive antagonist of the N-methyl-D-aspartate receptor (NMDA receptor), entering the channel of the receptor after it has been activated and thereby blocking the flow of ions. The NMDA receptor channels play an important role in synaptic plasticity and synapse formation underlying memory, learning and formation of neural networks during development in the central nervous system (CNS).
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These medications have the opposite action on the GnRH receptor but paradoxically have the same therapeutic effects. GnRH agonists, such as leuprorelin (Lupron), goserelin (Zoladex), and buserelin (Suprefact), are GnRH receptor superagonists, and work by producing profound desensitization of the GnRH receptor such that the receptor becomes non- functional. This occurs because GnRH is normally released in pulses, but GnRH agonists are continuously present, and this results in excessive downregulation of the receptor and ultimately a complete loss of function. At the initiation of treatment, GnRH agonists are associated with a "flare" effect on hormone levels due to acute overstimulation of the GnRH receptor.
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Psychosine receptor is a G protein-coupled receptor (GPCR) protein that in humans is encoded by the GPR65 gene. GPR65 is also referred to as TDAG8.
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C5a anaphylatoxin chemotactic receptor C5a2 also known as C5L2, G protein- coupled receptor 77, is a protein that in humans is encoded by the C5AR2 gene.
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The folate receptor gamma is a protein, that in humans is encoded by the FOLR3 gene. It is one of three isoforms to the folate receptor.
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One significant difference of the bidentate receptor was that there was no anion-arene stabilizing influence, and operated through purely chalcogen bonding, unlike the monodentate receptor.
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Nuclear receptor-interacting protein 1 (NRIP1) also known as receptor- interacting protein 140 (RIP140) is a protein that in humans is encoded by the NRIP1 gene.
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The muscarinic acetylcholine receptor M4, also known as the cholinergic receptor, muscarinic 4 (CHRM4), is a protein that, in humans, is encoded by the CHRM4 gene.
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The glycine receptor, alpha 4, also known as GLRA4, is a human pseudogene. The protein encoded by this gene is a subunit of the glycine receptor.
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Tumor necrosis factor receptor superfamily member 12A also known as the TWEAK receptor (TWEAKR) is a protein that in humans is encoded by the TNFRSF12A gene.
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GRIK4 (glutamate receptor, ionotropic, kainate 4) is a kainate receptor subtype belonging to the family of ligand-gated ion channels which is encoded by the gene.
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This peptide binds to bradykinin receptor B2 and its derivative, Des- Arg9-bradykinin binds to bradykinin receptor B1. Upon ligand binding, these receptors mediate inflammatory responses.
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SR-57227 is a potent and selective agonist at the 5HT3 receptor, with high selectivity over other serotonin receptor subtypes and good blood-brain barrier penetration.
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"The Neuropharmacology of Hallucinogens: a technical overview ". Erowid, v3.1 (August 2005). LSD, like many other drugs of recreational use, has been shown to activate DARPP-32-related pathways. The drug enhances dopamine D2 receptor protomer recognition and signaling of D2–5-HT2A receptor complexes, which may contribute to its psychotic effects. LSD has been shown to have low affinity for H1 receptors, displaying antihistamine effects. The crystal structure of LSD bound in its active state to a serotonin receptor, specifically the 5-HT2B receptor, has been elucidated for the first time in 2017. The LSD-bound 5-HT2B receptor is regarded as an excellent model system for the 5-HT2A receptor and the structure of the LSD- bound 5-HT2B receptor was used in the study as a template to determine the structural features necessary for the activity of LSD at the 5-HT2A receptor.
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Formyl peptide receptor 1 (FPR1, FPR1 receptor, fMet-Leu-Phe receptor 1, FMLP receptor 1, or N-formylmethionyl-leucyl-phenylalanine receptor 1) is a cell surface receptor protein that in humans is encoded by the formyl peptide receptor 1 (FPR1) gene. This gene encodes a G protein-coupled receptor cell surface protein that binds and is activated by N-Formylmethionine-containing oligopeptides, particularly N-Formylmethionine-leucyl-phenylalanine (FMLP). FPR1 is prominently expressed by mammalian phagocytic and blood leukocyte cells where it functions to mediate these cells' responses to the N-formylmethionine-containing oligopeptides which are released by invading microorganisms and injured tissues. FPR1 directs these cells to sites of invading pathogens or disrupted tissues and then stimulates these cells to kill the pathogens or to remove tissue debris; as such, it is an important component of the innate immune system that operates in host defense and damage control.
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While caffeine does not directly bind to any dopamine receptors, it influences the binding activity of dopamine at its receptors in the striatum by binding to adenosine receptors that have formed GPCR heteromers with dopamine receptors, specifically the A1–D1 receptor heterodimer (this is a receptor complex with 1 adenosine A1 receptor and 1 dopamine D1 receptor) and the A2A–D2 receptor heterotetramer (this is a receptor complex with 2 adenosine A2A receptors and 2 dopamine D2 receptors). The A2A–D2 receptor heterotetramer has been identified as a primary pharmacological target of caffeine, primarily because it mediates some of its psychostimulant effects and its pharmacodynamic interactions with dopaminergic psychostimulants. Caffeine also causes the release of dopamine in the dorsal striatum and nucleus accumbens core (a substructure within the ventral striatum), but not the nucleus accumbens shell, by antagonizing A1 receptors in the axon terminal of dopamine neurons and A1–A2A heterodimers (a receptor complex composed of 1 adenosine A1 receptor and 1 adenosine A2A receptor) in the axon terminal of glutamate neurons. During chronic caffeine use, caffeine-induced dopamine release within the nucleus accumbens core is markedly reduced due to drug tolerance.
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The nuclear receptor coactivator 2 also known as NCoA-2 is a protein that in humans is encoded by the NCOA2 gene. NCoA-2 is also frequently called glucocorticoid receptor-interacting protein 1 (GRIP1), steroid receptor coactivator-2 (SRC-2), or transcriptional mediators/intermediary factor 2 (TIF2).
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The nuclear receptor coactivator 3 also known as NCOA3 is a protein that, in humans, is encoded by the NCOA3 gene. NCOA3 is also frequently called 'amplified in breast 1' (AIB1), steroid receptor coactivator-3 (SRC-3), or thyroid hormone receptor activator molecule 1 (TRAM-1).
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The amitraz-octopamine receptor interaction restrains these normal functions of the octopamine receptor. Therefore, it is efficient as an insect-pesticide. Still, resistance against amitraz can occur. A mutation can lead to a working version of the octopamine receptor but with an altered pesticide target side.
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Extracellular interaction with a tripartite receptor composed of gp130, WSX1, and CNTFR, as well as interaction with the formyl peptide receptor 2 (formylpeptide-like-1 receptor) have been published. Intracellular interaction with BAX, tBID, IGFBP3, and TRIM11 may also be required for the effects of humanin.
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This gene encodes a member of the G protein-coupled receptor family, as well as the EDG family of proteins. This protein functions as a cellular receptor for lysophosphatidic acid and mediates lysophosphatidic acid-evoked calcium mobilization. This receptor couples predominantly to G(q/11) alpha proteins.
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The interleukin-18 receptor (IL-18R) is an interleukin receptor of the immunoglobulin superfamily. Endometrial IL-18 receptor mRNA and the ratio of IL-18 binding protein to interleukin 18 are significantly increased in adenomyosis patients in comparison to normal people, indicating a role in its pathogenesis.
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IL-10 has been shown to interact with Interleukin 10 receptor, alpha subunit. The receptor complex for IL-10 also requires the IL10R2 chain to initiate signalling. This ligand–receptor combination is found in birds and frogs, and is also likely to exist in bony fish.
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Hormone receptor antagonists bind to the normal receptor for a given hormone and prevent its activation. The target receptor may be on the cell surface, as in the case of peptide and glycoprotein hormones, or it may be intracellular, as in the case of steroid hormone receptors.
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G protein-coupled receptor family C group 6 member A (GPRC6A) is a protein that in humans is encoded by the GPRC6A gene. This protein functions as a receptor of L-α-amino acids, cations (e.g., calcium), osteocalcin, and steroids. It is a membrane androgen receptor.
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Nuclear receptor TLX (homologue of the Drosophila tailless gene) also known as NR2E1 (Nuclear receptor subfamily 2 group E member 1) is a protein that in humans is encoded by the NR2E1 gene. TLX is a member of the nuclear receptor family of intracellular transcription factors.
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When mice experienced vinclozolin exposure in utero, male offspring exhibited up-regulated estrogen receptor and up-regulated progesterone receptor. In females, vinclozolin down- regulated expression of estrogen receptors and up-regulated progesterone receptor expression. This result causes virilization and the feminization of males and masculinization of females.
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Orexin receptor type 1 (Ox1R or OX1), also known as hypocretin receptor type 1 (HcrtR1), is a protein that in humans is encoded by the HCRTR1 gene.
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Orexin receptor type 2 (Ox2R or OX2), also known as hypocretin receptor type 2 (HcrtR2), is a protein that in humans is encoded by the HCRTR2 gene.
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17β-Estradiol has been shown to activate the G protein-coupled receptor GPR30. However the subcellular localization and role of this receptor are still object of controversy.
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She has been vocal about popularizing the healing apoptotic effect of cannabinoids on cannabinoid receptor containing cancer cells while leaving the healthy cannabinoid receptor containing cells be.
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The PAK6 was originally cloned as an androgen receptor interacting kinase which can be stimulated by androgen receptor but not Rac or Cdc42, like other family members.
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Nitromifene has been found to dissociate from the estrogen receptor 250-fold faster than estradiol. This may be involved in its antagonistic activity at the estrogen receptor.
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Affinity is a measure of the tendency of a ligand to bind to its receptor. Efficacy is the measure of the bound ligand to activate its receptor.
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Growth factor receptor-bound protein 10 also known as insulin receptor-binding protein Grb-IR is a protein that in humans is encoded by the GRB10 gene.
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Almorexant is a competitive, dual OX1 and OX2 receptor antagonist and selectively inhibits the functional consequences of OX1 and OX2 receptor activation, such as intracellular Ca2+ mobilization.
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5-hydroxytryptamine (serotonin) receptor 3B, also known as HTR3B, is a human gene. The protein encoded by this gene is a subunit of the 5-HT3 receptor.
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According to a recent study, lactisole acts on a sweet taste receptor heteromer of the TAS1R3 sweet protein receptor in humans, but not on its rodent counterpart.
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Interleukin 5 receptor, alpha (IL5RA) also known as CD125 (Cluster of Differentiation 125) is a subunit of the Interleukin-5 receptor. IL5RA also denotes its human gene.
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Bupropion is known to weakly inhibit the α1 adrenergic receptor, with a 14% potency of its dopamine uptake inhibition, and the H1 receptor, with a 9% potency.
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IL-10 binding induces STAT3 signalling via the phosphorylation of the cytoplasmic tails of IL-10 receptor 1 + IL-10 receptor 2 by JAK1 and Tyk2 respectively.
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AT-076 is a so-called opioid "pan" antagonist and is the first reasonably balanced antagonist known of all four opioid receptor types. It acts as a silent antagonist of all four of the opioid receptors, behaving as a competitive antagonist of the μ-opioid receptor (Ki = 1.67 nM) and δ-opioid receptor (Ki = 19.6 nM) and as a noncompetitive antagonist of the κ-opioid receptor (Ki = 1.14 nM) and nociceptin receptor (Ki = 1.75 nM). AT-076 was derived from the selective κ-opioid receptor antagonist JDTic via removal of the 3,4-dimethyl group of the trans-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine antagonist scaffold, which increased affinity for the nociceptin receptor by 10-fold and for the μ- and δ-opioid receptors by 3-6-fold.
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Fulvestrant is an antiestrogen which acts as an antagonist of the estrogen receptor (ER) and additionally as a selective estrogen receptor degrader (SERD). It works by binding to the estrogen receptor and making it more hydrophobic, which makes the receptor unstable and misfold, which in turn leads normal processes inside the cell to degrade it. In addition to its antiestrogenic activity, fulvestrant is an agonist of the G protein-coupled estrogen receptor (GPER), albeit with relatively low affinity (10–100 nM, relative to 3–6 nM for estradiol).
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Met-enkephalin is a potent agonist of the δ-opioid receptor, and to a lesser extent the μ-opioid receptor, with little to no effect on the κ-opioid receptor. It is through these receptors that met-enkephalin produces its opioid effects, such as analgesia and antidepressant-like effects. It is also the endogenous ligand of the opioid growth factor receptor (OGFR; formerly known as the ζ-opioid receptor), which plays a role in the regulation of tissue growth and regeneration; hence why met-enkephalin is sometimes called OGF instead.
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The PTGDR2 gene is located on human chromosome 11 at position q12.2 (i.e. 11q12.2). It consists of two introns and three exons and codes for a G protein coupled receptor (GPCR) composed of 472 amino acids. DP2, is related to members of the chemotactic factor class of GPCRs, sharing an amino acid sequence identity of 29% with the C5a receptor, Formyl peptide receptor 1, and Formyl peptide receptor 2 receptors. DP2 has little or no such amino acid sequence relationship to the eight other Prostanoid receptors (see Eicosanoid receptor#Prostenoid receptors).
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Receptor activator of nuclear factor κ B (RANK), also known as TRANCE receptor or TNFRSF11A, is a member of the tumor necrosis factor receptor (TNFR) molecular sub-family. RANK is the receptor for RANK-Ligand (RANKL) and part of the RANK/RANKL/OPG signaling pathway that regulates osteoclast differentiation and activation. It is associated with bone remodeling and repair, immune cell function, lymph node development, thermal regulation, and mammary gland development. Osteoprotegerin (OPG) is a decoy receptor for RANKL, and regulates the stimulation of the RANK signaling pathway by competing for RANKL.
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Cholesterol binds to and affects the gating of a number of ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium channel. Cholesterol also activates the estrogen- related receptor alpha (ERRα), and may be the endogenous ligand for the receptor. The constitutively active nature of the receptor may be explained by the fact that cholesterol is ubiquitous in the body. Inhibition of ERRα signaling by reduction of cholesterol production has been identified as a key mediator of the effects of statins and bisphosphonates on bone, muscle, and macrophages.
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The vitamin D receptor (VDR), also known as the calcitriol receptor and as NR1I1 (nuclear receptor subfamily 1, group I, member 1), is a member of the nuclear receptor family of transcription factors. Calcitriol, the active form of vitamin D, binds to the VDR, which then forms a heterodimer with the retinoid-X receptor. This then binds to hormone response elements on DNA resulting in expression or transrepression of specific gene products. The VDR not only regulates transcriptional responses but also involved in microRNA- directed post transcriptional mechanisms.
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The thyrotropin receptor (or TSH receptor) is a receptor (and associated protein) that responds to thyroid-stimulating hormone (also known as "thyrotropin") and stimulates the production of thyroxine (T4) and triiodothyronine (T3). The TSH receptor is a member of the G protein-coupled receptor superfamily of integral membrane proteins and is coupled to the Gs protein. It is primarily found on the surface of the thyroid epithelial cells, but also found on adipose tissue and fibroblasts. The latter explains the reason of the myxedema finding during Graves disease.
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Perception of sweetness in nectar evolved in hummingbirds during their genetic divergence from insectivorous swifts, their closest bird relatives. Although the only known sweet sensory receptor, called T1R2, is absent in birds, receptor expression studies showed that hummingbirds adapted a carbohydrate receptor from the T1R1-T1R3 receptor, identical to the one perceived as umami in humans, essentially repurposing it to function as a nectar sweetness receptor. This adaptation for taste enabled hummingbirds to detect and exploit sweet nectar as an energy source, facilitating their distribution across geographical regions where nectar-bearing flowers are available.
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When inactive the progesterone receptor, as for other steroid receptor, forms a complex consisting of itself, heat shock proteins (hsp70, hsp90) and immunophilins. Upon activation, due to hormone binding to ligand binding pocket, the receptor complex has been shown to dissociate, triggering nuclear import and giving the receptor the property of dimerisation (Fig. 3). In the nucleus the dimer interacts with progesterone hormone response element in the DNA causing upregulation or downregulation of the gene. Various studies have demonstrated that it affects expression of up to 100 different genes, depending on receptor isomer.
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Through diverse means, extracellular ligand binding will typically cause or stabilize receptor dimerization. This allows a tyrosine in the cytoplasmic portion of each receptor monomer to be trans-phosphorylated by its partner receptor, propagating a signal through the plasma membrane. The phosphorylation of specific tyrosine residues within the activated receptor creates binding sites for Src homology 2 (SH2) domain- and phosphotyrosine binding (PTB) domain- containing proteins. Specific proteins containing these domains include Src and phospholipase Cγ. Phosphorylation and activation of these two proteins on receptor binding lead to the initiation of signal transduction pathways.
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The 5-HT2C receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). It is a G protein- coupled receptor (GPCR) that is coupled to Gq/G11 and mediates excitatory neurotransmission. HTR2C denotes the human gene encoding for the receptor, that in humans is located at the X chromosome. As males have one copy of the gene and in females one of the two copies of the gene is repressed, polymorphisms at this receptor can affect the two sexes to differing extent.
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Caveolin 1 has been shown to interact with heterotrimeric G proteins, Src tyrosine kinases (Src, Lyn) and H-Ras, cholesterol, TGF beta receptor 1, endothelial NOS, androgen receptor, amyloid precursor protein, gap junction protein, alpha 1, nitric oxide synthase 2A, epidermal growth factor receptor, endothelin receptor type B, PDGFRB, PDGFRA, PTGS2, TRAF2, estrogen receptor alpha, caveolin 2, PLD2, Bruton's tyrosine kinase and SCP2. All these interactions are through a caveolin-scaffolding domain (CSD) within caveolin-1 molecule. Molecules that interact with caveolin-1 contain caveolin-binding motifs (CBM).
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The small heterodimer partner (SHP) also known as NR0B2 (nuclear receptor subfamily 0, group B, member 2) is a protein that in humans is encoded by the NR0B2 gene. SHP is a member of the nuclear receptor family of intracellular transcription factors. SHP is unusual for a nuclear receptor in that it lacks a DNA binding domain. Therefore, it is technically neither a transcription factor nor nuclear receptor but nevertheless it is still classified as such due to relatively high sequence homology with other nuclear receptor family members.
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The galanin receptor is a G protein-coupled receptor, or metabotropic receptor which binds galanin. Galanin receptors can be found throughout the peripheral and central nervous systems and the endocrine system. So far three subtypes are known to exist: GAL-R1, GAL-R2, and GAL-R3. The specific function of each subtype remains to be fully elucidated, although as of 2009 great progress is currently being made in this respect with the generation of receptor subtype- specific knockout mice, and the first selective ligands for galanin receptor subtypes.
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Tropomyosin receptor kinase A (TrkA), also known as high affinity nerve growth factor receptor, neurotrophic tyrosine kinase receptor type 1, or TRK1-transforming tyrosine kinase protein is a protein that in humans is encoded by the NTRK1 gene. This gene encodes a member of the neurotrophic tyrosine kinase receptor (NTKR) family. This kinase is a membrane-bound receptor that, upon neurotrophin binding, phosphorylates itself (autophosphorylation) and members of the MAPK pathway. The presence of this kinase leads to cell differentiation and may play a role in specifying sensory neuron subtypes.
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Dioxins and dioxin-like compounds are teratogens that exert their effects through the aryl hydrocarbon receptor (AhR) in conjunction with the receptor's binding partner, aryl hydrocarbon receptor nuclear translocator (ARNT). The protein encoded by this gene represses signal transduction by the AhR by competing with the arylhydrocarbon receptor for binding to the ARNT. Expression of the repressor is stimulated by the receptor/translocator heterodimer, thereby regulating receptor function through a negative feedback mechanism. In addition, the encoded protein can bind to nuclear factor-kappa B. The AhRR gene may act as a tumor suppressor.
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ORG-2058, also known as 16α-ethyl-21-hydroxy-19-norprogesterone, is a progestin of the 19-norprogesterone group which was never marketed. It has high affinity for the progesterone receptor (775% of that of progesterone) and has been used in scientific research to study the role of the progesterone receptor in the body. The drug has no affinity for the estrogen receptor or the glucocorticoid receptor (less than 0.2% of the affinities of estradiol and dexamethasone, respectively) and has slight affinity for the mineralocorticoid receptor, but less than that of progesterone.
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Bitopic ligands target an orthosteric binding sites and allosteric binding sites on the same receptor. In scientific research, bivalent ligands have been used to study receptor dimers and to investigate their properties. This class of ligands was pioneered by Philip S. Portoghese and coworkers while studying the opioid receptor system. Bivalent ligands were also reported early on by Micheal Conn and coworkers for the gonadotropin-releasing hormone receptor.
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The protein encoded by this gene is a member of the G protein-coupled receptor family 2. This protein is a receptor for parathyroid hormone (PTH). This receptor is more selective in ligand recognition and has a more specific tissue distribution compared to parathyroid hormone 1 receptor (PTH1R). It is activated by PTH but not by parathyroid hormone-like hormone (PTHLH) and is particularly abundant in the brain and pancreas.
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Further investigation into the expression patterns of the CB2 receptors revealed that CB2 receptor gene transcripts are also expressed in the brain, though not as densely as the CB1 receptor and located on different cells. Unlike the CB1 receptor, in the brain, CB2 receptors are found primarily on microglia. The CB2 receptor is expressed in some neurons within the central nervous system (e.g.; the brainstem), but the expression is very low.
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Acetylcholine receptor subunit beta is a protein that in humans is encoded by the CHRNB1 gene. The muscle acetylcholine receptor is composed of five subunits: two alpha subunits and one beta, one gamma, and one delta subunit. This gene encodes the beta subunit of the acetylcholine receptor. The acetylcholine receptor changes conformation upon acetylcholine binding leading to the opening of an ion-conducting channel across the plasma membrane.
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Tumor necrosis factor receptor superfamily, member 19, also known as TNFRSF19 and TROY is a human gene. The protein encoded by this gene is a member of the TNF-receptor superfamily. This receptor is highly expressed during embryonic development. It has been shown to interact with TNF receptor associated factor (TRAF) family members, and to activate c-Jun N-terminal kinases (JNK) signaling pathway when overexpressed in cells.
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The word is most commonly used in this context in biochemistry and toxicology: interference in the physiological action of a chemical substance by another having a similar structure. For instance, a receptor antagonist is an agent that reduces the response that a ligand produces when the receptor antagonist binds to a receptor on a cell. An example of this is the interleukin-1 receptor antagonist. The opposite of antagonism is synergy.
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Dextrallorphan (DXA) is an opioid derivative chemical of the morphinan class that is used in scientific research. It acts as a σ1 receptor agonist and NMDA receptor antagonist. It has no significant affinity for the σ2, μ-opioid, or δ-opioid receptor, or for the serotonin or norepinephrine transporter. As an NMDA receptor antagonist, in vivo, it is approximately twice as potent as dextromethorphan, and five-fold less potent than dextrorphan.
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Allosteric modulators can alter the affinity and efficacy of other substances acting on a receptor. A modulator may also increase affinity and lower efficacy or vice versa. Affinity is the ability of a substance to bind to a receptor. Efficacy is the ability of a substance to activate a receptor, given as a percentage of the ability of the substance to activate the receptor as compared to the receptor's endogenous agonist.
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USP18 inhibits IFN-I signaling by disrupting the receptor complex and the subsequent JAK-STAT signaling pathway. USP18 binds the IFN-receptor 2 subunit (IFNAR2), leading to the displacement of Janus kinase 1. and the dissociation of the cytokine- receptor complex. This process requires STAT2 to traffic USP18 to the receptor These events terminate signaling and draw cells into a refractory state with diminished sensitivity to future stimulation.
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Fig 3. Binding sites of different therapeutic chemical groups on a GABAA receptor The GABAA receptors are made up of subunits which form a receptor complex. Humans have 19 receptor subunits and are classified into α (1–6), β (1–3), γ (1–3), δ, ε, π, θ, and ρ (1−3). The function of the receptor is different according to how the pentameric complex is put together.
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The mechanism by which neurosteroid GABAA receptor PAMs like brexanolone have antidepressant effects is unknown. Other GABAA receptor PAMs, such as benzodiazepines, are not known to have antidepressant effects. Neurosteroid GABAA receptor PAMs are known to interact with GABAA receptors and sub-populations differently than benzodiazepines. As examples, GABAA receptor-potentiating neurosteroids may preferentially target δ subunit-containing GABAA receptors, and enhance both tonic and phasic inhibition mediated by GABAA receptors.
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MAGE-A11 likely links transcriptionally active androgen receptor dimers. The MAGE-A11 dependent increase in androgen receptor transcriptional activity is mediated by a direct interaction of MAGE-A11 and transcriptional intermediary factor 2 (TIF2), suggesting that MAGE-A11 may act as a bridging factor to recruit other androgen receptor coactivators. Mutations in the androgen receptor that interfere with binding of MAGE-A11 can cause partial androgen insensitivity syndrome.
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The alpha-3 beta-4 nicotinic receptor, also known as the α3β4 receptor and the ganglion-type nicotinic receptor,Pharmacology, (Rang, Dale, Ritter & Moore, , 5th ed., Churchill Livingstone 2003) p. 138. is a type of nicotinic acetylcholine receptor, consisting of α3 and β4 subunits. It is located in the autonomic ganglia and adrenal medulla, where activation yields post- and/or presynaptic excitation, mainly by increased Na+ and K+ permeability.
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Endocytosis occurs as a result of a series of events. This begins when CMG2 or TEM8 is palmitoylated, which inhibits the association of the receptor with lipid rafts. This inhibits the receptor from being endocytosed before PA83 is cleaved and before LF or EF can associate with the heptamer. Reassociation of the receptor with the cholesterol and glycosphigolipid-rich microdomains (lipid rafts) occurs when PA63 binds to the receptor and heptamerizes.
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GPR182 (or G protein-coupled receptor 182) is a human gene (and associated protein) which is an orphan G-protein coupled receptor. When this gene was first cloned, it was proposed to encode an adrenomedullin receptor. However, when the corresponding protein was expressed, it was found not to respond to adrenomedullin (ADM). It was subsequently shown that a different GPCR, CALCRL when complexed with RAMP2 can function as an ADM receptor.
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There are two main types of estrogen receptors: estrogen receptor alpha (ERα) also known as NR3B1, and estrogen receptor beta (ER-β) also known as NR3A2. Both of these are nuclear receptors activated by the sex hormone, estrogen, and encoded by the ESR1 (Estrogen Receptor 1) gene. The estrogen signaling can be stimulated or inhibited selectively. This is dependent upon the equilibrium of these 2 receptor types in target organs.
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The progressive symptoms of anatoxin-a exposure are loss of coordination, twitching, convulsions and rapid death by respiratory paralysis. The nerve tissues which communicate with muscles contain a receptor called the nicotinic acetylcholine receptor. Stimulation of these receptors causes a muscular contraction. The anatoxin-a molecule is shaped so it fits this receptor, and in this way it mimics the natural neurotransmitter normally used by the receptor, acetylcholine.
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The complex central receptor is the G protein-coupled receptor calcitonin receptor-like receptor (CALCRL) which is necessary for CGRP and adrenomedullin (AM receptors). For function CGRP, CALCRL must coincide with RAMP1 where the ligand-binding domain of CGRP is located. It also includes two cytoplasmic proteins that associate with the CALCRL-RAMP1 to form signal transduction. CALCRL contains the Gα subunit, which activates adenylyl cyclase and cAMP-dependent signaling pathways.
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This gene encodes a member of the G protein-coupled receptor (GPCR) superfamily. This protein functions as a cell surface receptor for bile acids. Treatment of cells expressing this GPCR with bile acids induces the production of intracellular cAMP, activation of a MAP kinase signaling pathway, and internalization of the receptor. The receptor is implicated in the suppression of macrophage functions and regulation of energy homeostasis by bile acids.
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Cysteinyl leukotriene receptor 2, also termed CYSLTR2, is a receptor for cysteinyl leukotrienes (LT) (see leukotrienes#Cysteinyl leukotrienes). CYSLTR2, by binding these cysteinyl LTs (CysLTs; viz, LTC4, LTD4, and to a much lesser extent, LTE4) contributes to mediating various allergic and hypersensitivity reactions in humans. However, the first discovered receptor for these CsLTs, cysteinyl leukotriene receptor 1 (CysLTR1), appears to play the major role in mediating these reactions.
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Important steps in vitamin D mediated transcriptional regulation include 1) binding of vitamin D on its cognate vitamin D receptor (VDR), 2) the translocation of vitamin D receptor (VDR)-retinoid X receptor heterodimer complex in the nucleus, 3) binding VDR-RXR complex on the TRPV6 gene promoter, 4) recruitment of steroid receptor coactivator 1 and RNA polymerase II on the promoter, and 5) transcriptional activation mediated through histone H4 acetylation events.
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Pharmacodynamic tolerance begins when the cellular response to a substance is reduced with repeated use. A common cause of pharmacodynamic tolerance is high concentrations of a substance constantly binding with the receptor, desensitizing it through constant interaction. Other possibilities include a reduction in receptor density (usually associated with receptor agonists), or other mechanisms leading to changes in action potential firing rate. Pharmacodynamic tolerance to a receptor antagonist involves the reverse, i.e.
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An antagonist drug is one that attaches (or binds) to a site called a receptor without activating that receptor to produce a biological response. It is therefore said to have no intrinsic activity. An antagonist may also be called a receptor "blocker" because they block the effect of an agonist at the site. The pharmacological effects of an antagonist, therefore, result in preventing the corresponding receptor site's agonists (e.g.
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The gene encodes a protein which is one of several receptor subtypes for adenosine. The activity of the encoded protein, a G protein-coupled receptor family member, is mediated by G proteins which activate adenylyl cyclase, which induce synthesis of intracellular cAMP. The A2A receptor binds with the Gs protein at the intracellular site of the receptor. The Gs protein consists of three subunits; Gsα, Gsβ and Gsγ.
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The D1 subtype of the dopamine receptor is the most abundant dopamine receptor in the central nervous system. This G-protein coupled receptor is Gs/a coupled and indirectly activates cyclic AMP-dependent protein kinase, stimulating the neuron. D1 receptors regulate neuronal growth and development, mediate some behavioral responses, and modulate dopamine receptor D2-mediated events. Alternative transcription initiation sites result in two transcript variants of the gene.
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Receptor tyrosine-protein kinase erbB-3, also known as HER3 (human epidermal growth factor receptor 3), is a membrane bound protein that in humans is encoded by the ERBB3 gene. ErbB3 is a member of the epidermal growth factor receptor (EGFR/ERBB) family of receptor tyrosine kinases. The kinase-impaired ErbB3 is known to form active heterodimers with other members of the ErbB family, most notably the ligand binding-impaired ErbB2.
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GABAA receptor function is inhibited by zinc ions. The ions bind allosterically to the receptor, a mechanism that is critically dependent on the receptor subunit composition. De novo heterozygous missense mutations within a highly conserved region of the GABRB3 gene can decrease the peak current amplitudes of neurons or alter the kinetic properties of the channel. This results in the loss of the inhibitory properties of the receptor.
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EVH1 domain interacts with PPXXF motif. This sequence motif exists in group 1 metabotrophic glutamate receptor (mGluR1 and mGluR5), IP3 receptors (IP3R), Shank, transient receptor potential canonical (TRPC) family channels, drebrin, oligophrenin, dynamin3, CENTG1, and ryanodin receptor. Through its tetrameric structure, long forms of Homer (such as Homer1b and Homer1c) are proposed to cross link different proteins. For example, group 1 mGluR is crossed linked with its signaling downstream, IP3 receptor.
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The gamma-aminobutyric acid A receptor (GABAA receptor) is a multisubunit chloride channel that mediates the fastest inhibitory synaptic transmission in the central nervous system. This gene encodes GABA A receptor, beta 1 subunit. It is mapped to chromosome 4p12 in a cluster of genes encoding alpha 4, alpha 2 and gamma 1 subunits of the GABAA receptor. Alteration of this gene is implicated in the pathogenetics of schizophrenia.
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The protein encoded by this gene is a member of the TNF-receptor superfamily. This receptor is expressed preferentially by activated and antigen-experienced T lymphocytes. TNFRSF25 is also highly expressed by FoxP3 positive regulatory T lymphocytes. TNFRSF25 is activated by a monogamous ligand, known as TL1A (TNFSF15), which is rapidly upregulated in antigen presenting cells and some endothelial cells following Toll-Like Receptor or Fc receptor activation.
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A majority of growth factor receptors consists of receptor tyrosine kinases (RTKs). There are 3 dominant receptor types that are exclusive to research : the epidermal growth factor receptor, the neurotrophin receptor, and the insulin receptors. All growth factor receptors are membrane bound and composed of 3 general protein domains: extracellular, transmembrane, and cytoplasmic. The extracellular domain region is where a ligand may bind, usually with very high specificity.
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The protein encoded by this gene is a member of the TNF-receptor superfamily. This receptor contains an extracellular TRAIL-binding domain and a transmembrane domain, but no cytoplasmic death domain. This receptor is not capable of inducing apoptosis, and is thought to function as an antagonistic receptor that protects cells from TRAIL-induced apoptosis. This gene was found to be a p53-regulated DNA damage-inducible gene.
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The mode of signaling via the soluble Interleukin-6 receptor has been named Interleukin-6 trans-signaling whereas Interleukin-6 signaling via the membrane-bound Interleukin-6 receptor is referred to as Interleukin-6 classic signaling. Therefore, the generation of the soluble Interleukin-6 receptor enables cells to respond to Interleukin-6, which in the absence of soluble Interleukin-6 receptor would be completely unresponsive to the cytokine.
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BD1031 or (R)-2-[2-(3,4-dichlorophenyl)ethyl]octahydropyrrolo[1,2-a]pyrazine is a selective sigma receptor agonist, with a reported binding affinity of Ki = 1 ± 0.2 nM for the sigma-1 receptor and 80 times selectivity over the sigma-2 receptor. The enantiomer of BD1031 is known as BD1018. Consistent with other reported sigma receptor agonists, BD1031 increases the behavioural toxicity of cocaine in Swiss Webster mice.
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The H1 receptor is a histamine receptor belonging to the family of rhodopsin- like G-protein-coupled receptors. This receptor is activated by the biogenic amine histamine. It is expressed in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. The H1 receptor is linked to an intracellular G-protein (Gq) that activates phospholipase C and the inositol triphosphate (IP3) signalling pathway.
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Humans have far fewer active odor receptor genes than other primates and other mammals. In mammals, each olfactory receptor neuron expresses only one functional odor receptor. Odor receptor nerve cells function like a key–lock system: if the airborne molecules of a certain chemical can fit into the lock, the nerve cell will respond. There are, at present, a number of competing theories regarding the mechanism of odor coding and perception.
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Another Gi coupled human muscarinic receptor, M2, was also mutated to obtain the DREADD receptor hM2D. Another inhibitory Gi- DREADD is the kappa-opioid-receptor (KOR) DREADD (KORD) which is selectively activated by salvinorin B (SALB). Gs-coupled DREADDs have also been developed. These receptors are also known as GsD and are chimeric receptors containing intracellular regions of the turkey erythrocyte β-adrenergic receptor substituted into the rat M3 DREADD.
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The first radio-receptor assay (RRA) was done in 1970 by Lefkowitz et al., using a radiolabeled hormone to determine the binding affinity for its receptor. A radio-receptor assay requires the separation of the bound from the free ligand. This is done by filtration, centrifugation or dialysis.
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In some receptor systems (e.g. acetylcholine at the neuromuscular junction in smooth muscle), agonists are able to elicit maximal response at very low levels of receptor occupancy (<1%). Thus, that system has spare receptors or a receptor reserve. This arrangement produces an economy of neurotransmitter production and release.
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Most studies have looked at the receptor tyrosine kinases and examples of these are platelet derived growth factor receptor (PDGFR) pathway and epidermal growth factor receptor (EGFR). Src contains at least three flexible protein domains, which, in conjunction with myristoylation, can mediate attachment to membranes and determine subcellular localization.
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B-cell maturation antigen (BCMA or BCM), also known as tumor necrosis factor receptor superfamily member 17 (TNFRSF17), is a protein that in humans is encoded by the TNFRSF17 gene. TNFRSF17 is a cell surface receptor of the TNF receptor superfamily which recognizes B-cell activating factor (BAFF).
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Protease-activated receptor 4 (PAR-4), also known as coagulation factor II (thrombin) receptor-like 3, is a protein that in humans is encoded by the F2RL3 gene.
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This gene encodes alpha-1D-adrenergic receptor. Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a single intron that interrupts the coding region.
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BRI1-associated receptor kinase 1 (BAK1- also known as somatic embryogenesis receptor kinase 3 or SERK3) is an important plant protein that has diverse functions in plant development.
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Oxytocin receptor antagonists, such as barusiban or atosiban have the opposite effect of depressing oxytocin receptor activity and can be used to stop premature labor and uterine contractions.
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DOC acts as a selective 5-HT2A, 5-HT2B, and 5-HT2C receptor partial agonist. Its psychedelic effects are mediated via its actions on the 5-HT2A receptor.
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The heptapeptide angiotensin (1-7) also potentiates bradykinin action on B2 receptors. Kallidin also signals through the B2 receptor. An antagonist for the receptor is Hoe 140 (icatibant).
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Hsp72 together with Hsp90 form a heterocomplex with the estrogen receptor. Hence AFPep through interaction with Hsp72 controls the ligand binding and transcriptional activation of the estrogen receptor.
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Such an increase in the expression of a protein that virtually functions as a receptor is expected to occur when the specific signal for the receptor is missing.
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IL-7 receptor and signaling, common γ chain (blue) and IL-7 receptor-α (green) IL-7 binds to the IL-7 receptor, a heterodimer consisting of Interleukin-7 receptor alpha and common gamma chain receptor. Binding results in a cascade of signals important for T-cell development within the thymus and survival within the periphery. Knockout mice which genetically lack IL-7 receptor exhibit thymic atrophy, arrest of T-cell development at the double positive stage, and severe lymphopenia. Administration of IL-7 to mice results in an increase in recent thymic emigrants, increases in B and T cells, and increased recovery of T cells after cyclophosphamide administration or after bone marrow transplantation.
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As a result, the IUPHAR has recommended that the terms "BZ receptor", "GABA/BZ receptor" and "omega receptor" no longer be used and that the term "benzodiazepine receptor" be replaced with "benzodiazepine site". In order for GABAA receptors to be sensitive to the action of benzodiazepines they need to contain an α and a γ subunit, between which the benzodiazepine binds. Once bound, the benzodiazepine locks the GABAA receptor into a conformation where the neurotransmitter GABA has much higher affinity for the GABAA receptor, increasing the frequency of opening of the associated chloride ion channel and hyperpolarising the membrane. This potentiates the inhibitory effect of the available GABA leading to sedative and anxiolytic effects.
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Sketch of an enzyme-linked receptor structure (structure of IGF-1R) (click to enlarge) As of 2009, there are 6 known types of enzyme-linked receptors: Receptor tyrosine kinases; Tyrosine kinase associated receptors; Receptor-like tyrosine phosphatases; Receptor serine/threonine kinases; Receptor guanylyl cyclases and histidine kinase associated receptors. Receptor tyrosine kinases have the largest population and widest application. The majority of these molecules are receptors for growth factors such as epidermal growth factor (EGF), platelet- derived growth factor (PDGF), fibroblast growth factor (FGF), hepatocyte growth factor (HGF), nerve growth factor (NGF) and hormones such as insulin. Most of these receptors will dimerize after binding with their ligands, in order to activate further signal transductions.
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In the absence of hormone, estrogen receptors are largely located in the cytosol. Hormone binding to the receptor triggers a number of events starting with migration of the receptor from the cytosol into the nucleus, dimerization of the receptor, and subsequent binding of the receptor dimer to specific sequences of DNA known as hormone response elements. The DNA/receptor complex then recruits other proteins that are responsible for the transcription of downstream DNA into mRNA and finally protein that results in a change in cell function. Estrogen receptors also occur within the cell nucleus, and both estrogen receptor subtypes have a DNA-binding domain and can function as transcription factors to regulate the production of proteins.
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IGF-1 activates the insulin receptor at approximately 0.1 times the potency of insulin. Part of this signaling may be via IGF1R/Insulin Receptor heterodimers (the reason for the confusion is that binding studies show that IGF1 binds the insulin receptor 100-fold less well than insulin, yet that does not correlate with the actual potency of IGF1 in vivo at inducing phosphorylation of the insulin receptor, and hypoglycemia). IGF-1 binds and activates its own receptor, IGF-1R, through the cell surface expression of Receptor Tyrosine Kinase's (RTK's) and further signal through multiple intracellular transduction cascades. IGF-1R is the critical role-playing inducer in modulating the metabolic effects of IGF-1 for cellular senescence and survival.
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Many antagonists are reversible antagonists that, like most agonists, will bind and unbind a receptor at rates determined by receptor-ligand kinetics. Irreversible antagonists covalently bind to the receptor target and, in general, cannot be removed; inactivating the receptor for the duration of the antagonist effects is determined by the rate of receptor turnover, the rate of synthesis of new receptors. Phenoxybenzamine is an example of an irreversible alpha blocker—it permanently binds to α adrenergic receptors, preventing adrenaline and noradrenaline from binding. Inactivation of receptors normally results in a depression of the maximal response of agonist dose-response curves and a right shift in the curve occurs where there is a receptor reserve similar to non-competitive antagonists.
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G protein-coupled receptor 1, also known as GPR1, is a protein that in humans is encoded by the GPR1 gene. GPR1 is a member of the G protein-coupled receptor family of transmembrane receptors. It functions as a receptor for chemerin. Other receptors for chemerin include CMKLR1 and CCRL2.
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There exist two primary CNS cannabinoid receptors, on which marijuana and the cannabinoids act. Both the CB1 receptor and CB2 receptor are found in the brain. The CB2 receptor is also found in the immune system. CB1 is expressed at high densities in the basal ganglia, cerebellum, hippocampus, and cerebral cortex.
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The somatostatin analogue affects biodistribution of the radionuclide, and therefore how effectively any treatment effect can be targeted. Changes affect which somatostatin receptor is most strongly targeted. For example, DOTA- lanreotide (DOTALAN) has a lower affinity for receptor 2 and a higher affinity for receptor 5 compared to DOTA-octreotide (DOTATOC).
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Fibroblast growth factor receptor substrate 3 is a protein that in humans is encoded by the FRS3 gene. The protein encoded by this gene is a substrate for the fibroblast growth factor receptor. It is found in peripheral plasma membrane and functions in linking FGF receptor stimulation to activators of Ras.
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A selective progesterone receptor modulator (SPRM) is an agent that acts on the progesterone receptor (PR), the biological target of progestogens like progesterone. A characteristic that distinguishes such substances from full receptor agonists (e.g., progesterone, progestins) and full antagonists (e.g., aglepristone) is that their action differs in different tissues, i.e.
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The interleukin-27 receptor is a type I cytokine receptor for interleukin-27. It is a heterodimer composed of the interleukin 27 receptor, alpha subunit and glycoprotein 130. IL27RA essential for transcriptional activation of STAT1 and for augmenting the induction of T-bet expression during initiation of Th1 cell differentiation.
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In addition, the first 8 residues of the CXCL12 N-terminal serve as a receptor binding site, though only Lys-1 and Pro-2 directly participated in activating the receptor. Meanwhile, the RFFESH motif (residues 12-17) in the loop region function as a docking site for CXCL12 receptor binding.
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The sigma σ2 receptor was discovered and named in 1990, and was identified in part due to the dramatically reduced affinity of alazocine for the receptor relative to the σ1 receptor (in contrast to non-selective ligands like haloperidol, ditolylguanidine, and (+)-3-PPP, which show similar affinity for both subtypes).
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A second rhodopsin based structural model of the H4 receptor was successfully used for the identification of novel H4 ligands. Recent advancements in GPCR crystallization, in particular the determination of the human histamine H1 receptor in complex with doxepin will likely increase the quality of novel structural H4 receptor models.
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ER-X is a membrane-associated receptor that is bound and activated by 17α-estradiol and 17β-estradiol and is a putative membrane estrogen receptor (mER). It shows sequence homology with ERα and ERβ and activates the MAPK/ERK pathway. The receptor is insensitive to the antiestrogen ICI-182,780 (fulvestrant).
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Fibroblast growth factor receptor 1 (FGFR1), also known as basic fibroblast growth factor receptor 1, fms-related tyrosine kinase-2 / Pfeiffer syndrome, and CD331, is a receptor tyrosine kinase whose ligands are specific members of the fibroblast growth factor family. FGFR1 has been shown to be associated with Pfeiffer syndrome.
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Role of CD74 receptor in tissue injury and wound repair CD74 receptor is expressed on the surface of different cell types. Interaction between MIF cytokine and its cell membrane receptor CD74 activates pro-survival and proliferative pathways that protect against injury and promote healing in different parts of the body.
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Parathyroid hormone/parathyroid hormone-related peptide receptor, also known as parathyroid hormone 1 receptor (PTH1R), is a protein that in humans is encoded by the PTH1R gene. PTH1R functions as a receptor for parathyroid hormone (PTH) and for parathyroid hormone-related protein (PTHrP), also called parathyroid hormone-like hormone (PTHLH).
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Colony stimulating factor 1 receptor (CSF1R), also known as macrophage colony- stimulating factor receptor (M-CSFR), and CD115 (Cluster of Differentiation 115), is a cell-surface protein encoded, in humans, by the CSF1R gene (known also as c-FMS). It is a receptor for a cytokine called colony stimulating factor 1.
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The protein encoded by this gene is a member of the TNF-receptor superfamily. This receptor contains an extracellular TRAIL-binding domain, a transmembrane domain, and a truncated cytoplasmic death domain. This receptor does not induce apoptosis, and has been shown to play an inhibitory role in TRAIL- induced cell apoptosis.
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Ectodysplasin A receptor (EDAR) is a protein that in humans is encoded by the EDAR gene. EDAR is a cell surface receptor for ectodysplasin A which plays an important role in the development of ectodermal tissues such as the skin. It is structurally related to members of the TNF receptor superfamily.
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Interleukin-7 receptor subunit alpha (IL7R-α) also known as CD127 (Cluster of Differentiation 127) is a protein that in humans is encoded by the IL7R gene. IL7R-α is a type I cytokine receptor and is a subunit of the functional Interleukin-7 receptor and Thymic Stromal Lymphopoietin (TSLP) receptors.
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Incarvillateine's antinociceptive effect was blocked by the administration of adenosine receptor antagonists such as theophylline. This suggests that incarvillateine's main mechanism of action is mediated through the adenosine receptor.
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Probable G-protein coupled receptor 146 is a protein that in humans is encoded by the GPR146 gene. It has been identified as a possible receptor for C-peptide.
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Neuropeptide Y receptor type 2 (Y2R) is a member of the neuropeptide Y receptor family of G-protein coupled receptors, that in humans is encoded by the NPY2R gene.
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The triptan eletriptan is an agonist of the 5-HT1E receptor. BRL-54443 is a selective 5-HT1E and 5-HT1F receptor agonist which is used in scientific research.
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The renin receptor also known as ATPase H(+)-transporting lysosomal accessory protein 2, or the prorenin receptor, is a protein that in humans is encoded by the ATP6AP2 gene.
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These effects were completely inhibited by a selective 5-HT2C receptor antagonist, SB-242,084. Therefore, results suggest that YM348 is a potent and orally active 5-HT2C receptor agonist.
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Eptazocine (Sedapain) is an opioid analgesic which was introduced in Japan by Morishita in 1987. It acts as a mixed κ-opioid receptor agonist and μ-opioid receptor antagonist.
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Muscarine A muscarinic agonist is an agent that activates the activity of the muscarinic acetylcholine receptor. The muscarinic receptor has different subtypes, labelled M1-M5, allowing for further differentiation.
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The histamine H4 receptor, like the other three histamine receptors, is a member of the G protein-coupled receptor superfamily that in humans is encoded by the HRH4 gene.
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She found, through recombination analyses, that the spasmodic mutation maps to the Glra1 gene, coding for a glycine receptor subunit, and this point mutation decreases the glycine receptor function.
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Human secretin receptor (gene name SCTR) is a G protein-coupled receptor which binds secretin and is the leading member (i.e., first cloned) of the class B GPCR subfamily.
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Dextropropoxyphene acts as a mu-opioid receptor agonist. It also acts as a potent, noncompetitive α3β4 neuronal nicotinic acetylcholine receptor antagonist, as well as a weak serotonin reuptake inhibitor.
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Interleukin 10 receptor, alpha subunit is a subunit for the interleukin-10 receptor. IL10RA, is its human gene. IL10RA has also recently been designated CDW210A (cluster of differentiation W210A).
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It was then discovered that the blockage of the CB1 receptor represented a new pharmacological target. The first specific CB1 receptor antagonist / inverse agonist was rimonabant, discovered in 1994.
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The P2RX7 receptor is overexpressed in most malignant tumors. The expression of the adenosine A2A receptor on endothelial cells is upregulated in the early stages of human lung cancer.
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The bioavailability of lormetazepam was found to be 80%. Lormetazepam and other benzodiazepine drugs act as positive modulators at the GABAA benzodiazepine receptor complex. Lormetazepam binds to the benzodiazepine receptor which in turn enhances the effect of the GABAA receptor producing its therapeutic effects as well as adverse effects. When lormetazepam binds to the benzodiazepine receptor sites in sufficient quantities it produces sedation which is used clinically as a therapeutic treatment for insomnia.
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The mechanism for GLUT4 is an example of a cascade effect, where binding of a ligand to a membrane receptor amplifies the signal and causes a cellular response. In this case, insulin binds to the insulin receptor in its dimeric form and activates the receptor's tyrosine-kinase domain. The receptor then recruits Insulin Receptor Substrate, or IRS-1, which binds the enzyme PI-3 kinase. PI-3 kinase converts the membrane lipid PIP2 to PIP3.
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Plants have various mechanisms to perceive danger in their environment. Plants are able to detect pathogens and microbes through surface level receptor kinases (PRK). Additionally, receptor-like proteins (RLPs) containing ligand binding receptor domains capture pathogen-associated molecular patterns (PAMPS) and damage-associated molecular patterns (DAMPS) which consequently initiates the plant's innate immunity for a defense response. Plant receptor kinases are also used for growth and hormone induction among other important biochemical processes.
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Both receptor types bind and are activated by a series of formylated oligopeptide chemotactic factors but FLP2 receptor appears to be a promiscuous receptor in that it also binds to and is activated by lipoxins and resolvins as well as various polypeptides and proteins. The FLP2 receptor appears to be engaged primarily in dampening and resolving inflammation responses, actions which appear to be diametrically opposite to the pro-inflammatory actions of FLP1 receptors.
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C-X-C chemokine receptor type 5 (CXC-R5) also known as CD185 (cluster of differentiation 185) or Burkitt lymphoma receptor 1 (BLR1) is a G protein- coupled seven transmembrane receptor for chemokine CXCL13 (also known as BLC) and belongs to the CXC chemokine receptor family. It enables T cells to migrate to lymph node and the B cell zones. In humans, the CXC-R5 protein is encoded by the CXCR5 gene.
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Coronavirus replication cycle The attachment of the SARS-related coronavirus to the host cell is mediated by the spike protein and its receptor. The spike protein receptor binding domain (RBD) recognizes and attaches to the angiotensin-converting enzyme 2 (ACE2) receptor. Following attachment, the virus can enter the host cell by two different paths. The path the virus takes depends on the host protease available to cleave and activate the receptor-attached spike protein.
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Sunderland, MA: Sinauer Identification begins with an odorant binding to specific odorant receptor proteins. Olfactory receptor molecules are very similar to G-protein- linked receptors and belong to the odorant receptor gene family. The specificity of odor recognition is the result of the molecular variety of odorant receptor proteins and their interaction with the odorant molecules. However, the specific mechanism of certain receptors binding with certain odorant molecules is not well understood.
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Mammalian bombesin-like peptides are widely distributed in the central nervous system as well as in the gastrointestinal tract, where they modulate smooth-muscle contraction, exocrine and endocrine processes, metabolism, and behavior. They bind to G protein-coupled receptors on the cell surface to elicit their effects. Bombesin-like peptide receptors include gastrin-releasing peptide receptor, neuromedin B receptor, and bombesin-like receptor-3 (BRS3; this article). BB3 is a G protein-coupled receptor.
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Interleukin-31 receptor A is a protein that in humans is encoded by the IL31RA gene. IL31RA is related to gp130 (IL6ST; MIM 600694), the common receptor subunit for IL6 (MIM 147620)-type cytokines. Oncostatin M receptor (OSMR; MIM 601743) and IL31RA form the heterodimeric receptor through which IL31 (MIM 609509) signals. Expression of IL31RA and OSMR mRNA is induced in activated monocytes, and both mRNAs are constitutively expressed in epithelial cells (Dillon et al.
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Death receptor 6 (DR6), also known as tumor necrosis factor receptor superfamily member 21 (TNFRSF21), is a cell surface receptor of the tumor necrosis factor receptor superfamily which activates the JNK and NF-κB pathways. It is mostly expressed in the thymus, spleen and white blood cells. The Gene for DR6 is 78,450 bases long and is found on the 6th chromosome. This is transcribed into a 655 amino acid chain weighing 71.8 kDa.
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Serotype 2 (AAV2) has been the most extensively examined so far. AAV2 presents natural tropism towards skeletal muscles, neurons, vascular smooth muscle cells and hepatocytes. Three cell receptors have been described for AAV2: heparan sulfate proteoglycan (HSPG), aVβ5 integrin and fibroblast growth factor receptor 1 (FGFR-1). The first functions as a primary receptor, while the latter two have a co-receptor activity and enable AAV to enter the cell by receptor-mediated endocytosis.
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CCR5 receptor antagonists are a class of small molecules that antagonize the CCR5 receptor. The C-C motif chemokine receptor CCR5 is involved in the process by which HIV, the virus that causes AIDS, enters cells. Hence antagonists of this receptor are entry inhibitors and have potential therapeutic applications in the treatment of HIV infections. The life cycle of the HIV presents potential targets for drug therapy, one of them being the viral entry pathway.
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Binding to VEGF receptor induces dimerization, which modifies the conformation in the intracellular domain. This modification leads to the exposure of the ATP- binding site, which causes ATP binding on the receptor and also transphosphorylation on specific tyrosine residues. Tyrosine phosphorylation on the receptor is regulated by internalization, degradation and by dephosphorylation through different protein tyrosine phosphatases. This can then lead to the initial receptor signal transduction cascade, which activates several downstream enzymatic pathways.
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Umespirone (KC-9172) is a drug of the azapirone class which possesses anxiolytic and antipsychotic properties. It behaves as a 5-HT1A receptor partial agonist (Ki = 15 nM), D2 receptor partial agonist (Ki = 23 nM), and α1-adrenoceptor receptor antagonist (Ki = 14 nM), and also has weak affinity for the sigma receptor (Ki = 558 nM). Unlike many other anxiolytics and antipsychotics, umespirone produces minimal sedation, cognitive/memory impairment, catalepsy, and extrapyramidal symptoms.
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Tyrosine-protein kinase transmembrane receptor ROR2 also known as neurotrophic tyrosine kinase, receptor-related 2, is a protein that in humans is encoded by the ROR2 gene located on position 9 of the long arm of chromosome 9. This protein is responsible for aspects of bone and cartilage growth. It is involved in Robinow syndrome and autosomal dominant brachydactyly type B. ROR2 is a member of the receptor tyrosine kinase-like orphan receptor (ROR) family.
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GPR50 is a member of the G protein-coupled receptor family of integral membrane proteins and is most closely related to the melatonin receptor. GPR50 is able to heterodimerize with both the MT1 and MT2 melatonin receptor subtypes. While GPR50 has no effect on MT2 function, GPR50 prevented MT1 from both binding melatonin and coupling to G proteins. GPR50 is the mammalian ortholog of melatonin receptor Mel1c described in non-mammalian vertebrates.
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Alteration in the expression, distribution, autoregulation, and prevalence of specific glutamate heterodimers alters relative levels of paired G proteins to the heterodimer- forming glutamate receptor in question. Namely: 5HT2A and mGlu2 form a dimer which mediates psychotomimetic and entheogenic effects of psychedelics; as such this receptor is of interest in schizophrenia. Agonists at either constituent receptor may modulate the other receptor allosterically; e.g. glutamate-dependent signaling via mGlu2 may modulate 5HT2A-ergic activity.
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Different strains of HIV work on different co-receptors, although the virus can switch to utilizing other co-receptors. For example, R5X4 receptors can become the dominant HIV co-receptor target in main strains. HIV-1 and HIV-2 can both use the CCR8 co-receptor. The crossover of co-receptor targets for different strains and the ability for the strains to switch from their dominant co- receptor can impede clinical treatment of HIV.
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The receptor kinase properties of PEPR1 and PEPR2 allow them to perform important duties within plants. Plants have complex and detailed signaling systems, and receptor kinases ensure that these systems function properly. The receptor kinases recognize elements associated with pathogens that interact with the plant to ensure that the plant can protect itself from foreign, harmful substances. Using these properties, receptor kinases are very important in the immune system of a plant.
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By blocking AT1 receptors, ARBs lead to lower blood pressure. An insurmountable inhibition of the AT1 receptor is achieved when the maximum response of Ang II cannot be restored in the presence of the ARB, no matter how high the concentration of Ang II is. The angiotensin receptor blockers can inhibit the receptor in a competitive surmountable, competitive insurmountable or noncompetitive fashion, depending upon the rate at which they dissociate from the receptor.
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The incident-light calibration constant depends on the type of light receptor. Two receptor types are common: flat (cosine-responding) and hemispherical (cardioid-responding). With a flat receptor, ISO 2720:1974 recommends a range for C of 240 to 400 with illuminance in lux; a value of 250 is commonly used. A flat receptor typically is used for measurement of lighting ratios, for measurement of illuminance, and occasionally, for determining exposure for a flat subject.
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The N-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel protein found in nerve cells. The NMDA receptor is one of three types of ionotropic glutamate receptors. The other receptors are the AMPA and kainate receptors. It is activated when glutamate and glycine (or D-serine) bind to it, and when activated it allows positively charged ions to flow through the cell membrane.
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Memantine is an example of an uncompetitive channel blocker of the NMDA receptor, with a relatively rapid off-rate and low affinity. At physiological pH its amine group is positively charged and its receptor antagonism is voltage-dependent. It thereby mimics the physiological function of Mg2+ as channel blocker. Memantine only blocks NMDA receptor associated channels during prolonged activation of the receptor, as it occurs under excitotoxic conditions, by replacing magnesium at the binding site.
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Moxonidine is a selective agonist at the imidazoline receptor subtype 1 (I1). This receptor subtype is found in both the rostral ventro-lateral pressor and ventromedial depressor areas of the medulla oblongata. Moxonidine therefore causes a decrease in sympathetic nervous system activity and, therefore, a decrease in blood pressure. Compared to the older central-acting antihypertensives, moxonidine binds with much greater affinity to the imidazoline I1-receptor than to the α2-receptor.
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Metabolic regulation of glycogen by glucagon. Glucagon binds to the glucagon receptor, a G protein-coupled receptor, located in the plasma membrane. The conformation change in the receptor activates G proteins, a heterotrimeric protein with α, β, and γ subunits. When the G protein interacts with the receptor, it undergoes a conformational change that results in the replacement of the GDP molecule that was bound to the α subunit with a GTP molecule.
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Cedric Blanpain started his research career working on the CCR5 co-receptor which had been characterized by the Parmentier lab. He worked on understanding the function of the receptor and how the HIV interacts with it. The young researcher showed that endocytosis of the HIV is essential to the cell's infection. He was able to find the first chemokine antagonist to the receptor as well as antibodies that could mediate the oligomerization of the receptor.
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Entry mechanisms of Old World and New World arenaviruses. Lassa mammarenavirus gains entry into the host cell by means of the cell-surface receptor the alpha-dystroglycan (alpha-DG), a versatile receptor for proteins of the extracellular matrix. It shares this receptor with the prototypic Old World arenavirus lymphocytic choriomeningitis virus. Receptor recognition depends on a specific sugar modification of alpha-dystroglycan by a group of glycosyltransferases known as the LARGE proteins.
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Following tissue injury, the inflammatory response is a protective process to promote restoration of the tissue to homeostasis. Resolution of inflammation involves various specialized lipid mediators, including resolvins. Resolvins are under laboratory research for their potential to act through G protein-coupled receptors (GPRs): 1) RvD1 and AT- RvD1 act through the Formyl peptide receptor 2, which is also activated by certain lipoxins and is therefore often termed the ALX/FPR2 receptor; 2) RvD1, AT-RVD1, RvD3, AT-RvD3, and RvD5 act through the GPR32 receptor which is now also termed the RVD1 receptor; 3) RvD2 acts through the GPR18 receptor also now termed the RvD2 receptor; and 4) RvE1 and the 18(S) analog of RvE1 are full activators while RvE2 is a partial activator of the CMKLR1 receptor. All of these receptors activate their parent cells through standard GPR-mobilized pathways.
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The PGJ2 series of cyclopentenone PGs bind to and activate the G protein-coupled receptor, Prostaglandin DP2 receptor, with 15-deoxy-Δ12,14-PGJ2 and PDJ2 exhibiting potencies comparable to PGD2 (i.e. Ki equilibrium constants ~20-45 nanomolar) and Δ12-PGJ2 having 10-fold lesser potency, at least on mouse DP2 receptor. These PGJ2's also bind and activate a second G protein-coupled receptor, Prostaglandin DP1 receptor, but require high concentrations to do so; this activation is not considered physiological. DP2 and DP1 are G protein-coupled receptors, with the DP2 receptor coupled to Gi alpha subunit-dependent depression of cellular cAMP levels and causing the potentiation cell injury in neural tissue cultures and with the DP1 receptor coupled to Gs alpha subunit-dependent increases in cellular cAMP levels and the suppression of cell injury in neural tissue cultures.
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The GPR32 was initially identified and defined by molecular cloning in 1998 as coding for an orphan receptor, i.e. a protein with an amino acid sequence similar to known receptors but having no known ligand(s) to which it responds and no known function. The projected amino acid sequence of GPR32, however, shared 35-39% amino acid identity with certain members of the chemotactic factor receptor family, i.e. 39% identity with Formyl peptide receptor 1, which is a receptor for N-Formylmethionine- leucyl-phenylalanine and related N-formyl peptide chemotactic factors, and 35% identity with Formyl peptide receptor 2, which likewise is also a receptor for N-formyl peptides but also a receptor for certain lipoxins which are arachidonic acid metabolites belonging to a set of specialized proresolving mediators that act to resolve or inhibit inflammatory reactions.
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A melatonergic agent (or drug) is a chemical which functions to directly modulate the melatonin system in the body or brain. Examples include melatonin receptor agonists and melatonin receptor antagonists.
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Colquhoun D (1987). Affinity, efficacy and receptor classification: is the classical theory still useful? In Perspectives on hormone receptor classification, eds. Black JW, Jenkinson DH, & Gerskowitch VP, pp. 103–114.
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It has been shown to be a potent nicotinic receptor antagonist in animal models with an IC50 of 6µM at the α7 site and 13 nM for the α4β2 receptor.
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A third receptor has been discovered (VEGFR-3); however, VEGF-A is not a ligand for this receptor. VEGFR-3 mediates lymphangiogenesis in response to VEGF-C and VEGF-D.
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The speract receptor found in egg, is a transmembrane glycoprotein. Other members of this family include the macrophage scavenger receptor type I, an enteropeptidase, and T-cell surface glycoprotein CD5.
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CP-135807 is a drug which acts as a potent and selective agonist for the 5-HT1D serotonin receptor, and is used to study the function of this receptor subtype.
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5-hydroxytryptamine receptor 3C is a protein that in humans is encoded by the HTR3C gene. The protein encoded by this gene is a subunit of the 5-HT3 receptor.
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5-hydroxytryptamine receptor 3D is a protein that in humans is encoded by the HTR3D gene. The protein encoded by this gene is a subunit of the 5-HT3 receptor.
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5-hydroxytryptamine receptor 3E is a protein that in humans is encoded by the HTR3E gene. The protein encoded by this gene is a subunit of the 5-HT3 receptor.
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Glutamate receptor, ionotropic, N-methyl D-aspartate-like 1B, also known as GRINL1B, is a human gene. The protein encoded by this gene is a subunit of the NMDA receptor.
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Metabotropic glutamate receptor 5 is an excitatory Gq-coupled G protein- coupled receptor predominantly expressed on the postsynaptic sites of neurons. In humans, it is encoded by the GRM5 gene.
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Glutamate ionotropic receptor kainate type subunit 2, also known as ionotropic glutamate receptor 6 or GluR6, is a protein that in humans is encoded by the GRIK2 (or GLUR6) gene.
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Interleukin 17A and its receptor play a pathogenic role in many inflammatory and autoimmune diseases such as rheumatoid arthritis. Like other cytokine receptors, this receptor likely has a multimeric structure.
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CLEC9A is a group V C-type lectin-like receptor (CTLR) that functions as an activation receptor and is expressed on myeloid lineage cells (Huysamen et al., 2008 [PubMed 18408006]).
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Numa and co-workers cloned and sequenced the cDNA and delineated the primary structures of different families of receptors and channels including a neurotransmitter-gated channel (nicotinic acetylcholine receptor), voltage-gated channels (sodium channel and calcium channel), an intracellular membrane channel (calcium-release channel), and a G-protein- coupled receptor (muscarinic acetylcholine receptor).
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The neuromedin B receptor (NMBR), now known as BB1 is a G protein-coupled receptor whose endogenous ligand is neuromedin B. In humans, this protein is encoded by the NMBR gene. Neuromedin B receptor binds neuromedin B, a potent mitogen and growth factor for normal and neoplastic lung and for gastrointestinal epithelial tissue.
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USP20 is involved in the recycling of the β2-adrenergic receptor. After agonist stimulation, the receptor is internalised and ubiquitinated. USP20 serves to deubiquitinate the receptor and prevent its degradation by the proteasome. This allows it to be recycled to the cell surface in order to resensitize the cell to signalling molecules.
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Dendritic spines express glutamate receptors (e.g. AMPA receptor and NMDA receptor) on their surface. The TrkB receptor for BDNF is also expressed on the spine surface, and is believed to play a role in spine survival. The tip of the spine contains an electron-dense region referred to as the "postsynaptic density" (PSD).
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Receptors which initiate cell fate transduction cascades, in early embryo development, exhibit a ratchet effect in response to morphogen concentrations. The low receptor occupancy permits increases in receptor occupancy which alter the cell fate, but the high receptor affinity does not allow ligand dissociation leading to a cell fate of a lower concentration.
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Trace amine-associated receptor 5 is a protein that in humans is encoded by the TAAR5 gene. In vertebrates, TAAR5 is expressed in the olfactory epithelium. Human TAAR5 (hTAAR5) is a functional trace amine-associated receptor which acts as an olfactory receptor for tertiary amines. Trimethylamine and are full agonists of hTAAR5.
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CGS-12066A is a drug which acts as a potent and selective agonist for the 5-HT1B receptor with lower affinity for the three 5-HT2 receptor subtypes. It is used for studying the role of the 5-HT1B receptor in various processes including perception of pain and the sleep-wake cycle.
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Some alpha gliadin have other direct-acting properties. Other gliadin peptides, one in a glutamine rich region and another peptide, "QVLQQSTYQLLQELCCQHLW", bind a chemoattractant receptor, CXCR3. Gliadin binds to, blocks and displaces a factor, I-TAC, that binds this receptor. In the process it recruits more CXCR3 receptor, increases MyD88 and Zonulin expression.
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This receptor has been proposed as a target for treating sleep disorders. The receptor has also been proposed as a target for treating neuropathic pain. Because of its ability to modulate other neurotransmitters, H3 receptor ligands are being investigated for the treatment of numerous neurological conditions, including obesity (because of the histamine/orexinergic system interaction), movement disorders (because of H3 receptor-modulation of dopamine and GABA in the basal ganglia), schizophrenia and ADHD (again because of dopamine modulation) and research is underway to determine whether H3 receptor ligands could be useful in modulating wakefulness (because of effects on noradrenaline, glutamate and histamine).
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Agonist vs. antagonist In pharmacology the term agonist-antagonist or mixed agonist/antagonist is used to refer to a drug which under some conditions behaves as an agonist (a substance that fully activates the receptor that it binds to) while under other conditions, behaves as an antagonist (a substance that binds to a receptor but does not activate and can block the activity of other agonists). Types of mixed agonist/antagonist include receptor ligands that act as agonist for some receptor types and antagonist for others or agonist in some tissues while antagonist in others (also known as selective receptor modulators).
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Stefano traced the co-evolution of OR and the immune system underlying the fact that these receptors helped earlier animals to survive pain and inflammation shock in aggressive environments. The receptor families delta, kappa, and mu demonstrate 55–58% identity to one another, and a 48–49% homology to the nociceptin receptor. Taken together, this indicates that the NOP receptor gene, OPRL1, has equal evolutionary origin, but a higher mutation rate, than the other receptor genes. Even though opioid receptor families are similar to each other in many ways, their structural differences lead to differences in functionality.
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The epidermal growth factor receptor (EGFR; ErbB-1; HER1 in humans) is a transmembrane protein that is a receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligands. The epidermal growth factor receptor is a member of the ErbB family of receptors, a subfamily of four closely related receptor tyrosine kinases: EGFR (ErbB-1), HER2/neu (ErbB-2), Her 3 (ErbB-3) and Her 4 (ErbB-4). In many cancer types, mutations affecting EGFR expression or activity could result in cancer. Epidermal growth factor and its receptor was discovered by Stanley Cohen of Vanderbilt University.
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Camazepam, like others benzodiazepines, produce a variety of therapeutic and adverse effects by binding to the benzodiazepine receptor site on the GABAA receptor and modulating the function of the GABA receptor, the most prolific inhibitory receptor within the brain. The GABA chemical and receptor system mediates inhibitory or calming effects of camazepam on the nervous system. Compared to other benzodiazepines, it has reduced side effects such as impaired cognition, reaction times and coordination, which makes it best suited as an anxiolytic because of these reduced sides effects. Animal studies have shown camazepam and its active metabolites possess anticonvulsant properties.
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Polymeric IgA (mainly the secretory dimer) is produced by plasma cells in the lamina propria adjacent to mucosal surfaces. It binds to the polymeric immunoglobulin receptor on the basolateral surface of epithelial cells, and is taken up into the cell via endocytosis. The receptor-IgA complex passes through the cellular compartments before being secreted on the luminal surface of the epithelial cells, still attached to the receptor. Proteolysis of the receptor occurs, and the dimeric IgA molecule, along with a portion of the receptor known as the secretory component, are free to diffuse throughout the lumen.
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Montelucast is in use to treat various conditions including asthma, exercise-induced bronchoconstriction, allergic rhinitis, primary dysmenorrhoea (i.e. dysmenorrhoea not associated with known causes; see dysmenorrhea#causes), and urticaria. It has been presumed that this drug's beneficial effects in these diseases is due to its well-known ability to act as a receptor antagonist for the cysteinyl leukotriene receptor 1 (CysLTR1), i.e. it binds to but does not activate this receptor thereby interfering with LTD4, LTC4, and LTE4 provocative actions by blocking their binding to CysLTR1 (the drug does not block the cysteinyl leukotriene receptor 2) (see cysteinyl leukotriene receptor 1#Clinical significance).
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Retinoid X receptor beta (RXR-beta), also known as NR2B2 (nuclear receptor subfamily 2, group B, member 2) is a nuclear receptor that in humans is encoded by the RXRB gene. This gene encodes a member of the retinoid X receptor (RXR) family of nuclear receptors which are involved in mediating the effects of retinoic acid (RA). This receptor forms heterodimers with the retinoic acid, thyroid hormone, and vitamin D receptors, increasing both DNA binding and transcriptional function on their respective response elements. The gene lies within the major histocompatibility complex (MHC) class II region on chromosome 6.
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General pathways for GPCR homologous desensitization Homologous desensitization occurs when a receptor decreases its response to an agonist at high concentration. It is a process through which, after prolonged agonist exposure, the receptor is uncoupled from its signaling cascade and thus the cellular effect of receptor activation is attenuated. Homologous desensitization is distinguished from heterologous desensitization, a process in which repeated stimulation of a receptor by an agonist results in desensitization of the stimulated receptor as well as other, usually inactive, receptors on the same cell. They are sometimes denoted as agonist-dependent and agonist-independent desensitization respectively.
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Endothelin functions through activation of two G protein-coupled receptors, endothelinA and endothelinB receptor (ETA and ETB, respectively). These two subtypes of endothelin receptor are distinguished in the laboratory by the order of their affinity for the three endothelin peptides: the ETA receptor is selective for ET-1, whereas the ETB receptor has the same affinity for all three ET peptides. The two types of ET receptor are distributed across diverse cells and organs, but with different levels of expression and activity, indicating a multiple-organ ET system. Endothelin-1 is the most powerful endogenous chemical affecting vascular tone across organ systems.
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One notable example of functional selectivity occurs with the 5-HT2A receptor, as well as the 5-HT2C receptor. Serotonin, the main endogenous ligand of 5-HT receptors, is a functionally selective agonist at this receptor, activating phospholipase C (which leads to inositol triphosphate accumulation), but does not activate phospholipase A2, which would result in arachidonic acid signaling. However, the other endogenous compound dimethyltryptamine activates arachidonic acid signaling at the 5-HT2A receptor, as do many exogenous hallucinogens such as DOB and lysergic acid diethylamide (LSD). Notably, LSD does not activate IP3 signaling through this receptor to any significant extent.
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A receptor which is capable of producing a biological response in the absence of a bound ligand is said to display "constitutive activity". The constitutive activity of a receptor may be blocked by an inverse agonist. The anti-obesity drugs rimonabant and taranabant are inverse agonists at the cannabinoid CB1 receptor and though they produced significant weight loss, both were withdrawn owing to a high incidence of depression and anxiety, which are believed to relate to the inhibition of the constitutive activity of the cannabinoid receptor. The GABAA receptor has constitutive activity and conducts some basal current in the absence of an agonist.
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A number of pathogenic microorganisms, including C. albicans, Pneumocystis carinii and Leishmania donovani display glycans on their surfaces with terminal mannose residues that are recognised by the C-type CRDs of the mannose receptor, thereby acting as a marker of non-self. Upon recognition, the receptor internalises the bound pathogen and transports it to lysosomes for degradation via the phagocytic pathway. In this way, the mannose receptor acts as a pattern recognition receptor. The presence of a di-aromatic FENTLY (Phe-Glu-Asn-Thr-Leu-Tyr) sequence motif in the cytoplasmic tail of the receptor is vital for its clathrin-mediated internalization.
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TLRs are a type of pattern recognition receptor (PRR) and recognize molecules that are broadly shared by pathogens but distinguishable from host molecules, collectively referred to as pathogen-associated molecular patterns (PAMPs). TLRs together with the Interleukin-1 receptors form a receptor superfamily, known as the "interleukin-1 receptor / toll-like receptor superfamily"; all members of this family have in common a so-called TIR (toll- IL-1 receptor) domain. Three subgroups of TIR domains exist. Proteins with subgroup 1 TIR domains are receptors for interleukins that are produced by macrophages, monocytes, and dendritic cells and all have extracellular Immunoglobulin (Ig) domains.
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Several hypotheses are given about how tolerance develops, including opioid receptor phosphorylation (which would change the receptor conformation), functional decoupling of receptors from G-proteins (leading to receptor desensitization), μ-opioid receptor internalization or receptor down-regulation (reducing the number of available receptors for morphine to act on), and upregulation of the cAMP pathway (a counterregulatory mechanism to opioid effects) (For a review of these processes, see Koch and Hollt.) CCK might mediate some counter- regulatory pathways responsible for opioid tolerance. CCK-antagonist drugs, specifically proglumide, have been shown to slow the development of tolerance to morphine.
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NNC 63-0532 is a nociceptoid drug used in scientific research. It acts as a potent and selective agonist for the nociceptin receptor, also known as the ORL-1 (opiate receptor-like 1) receptor. The function of this receptor is still poorly understood, but it is thought to have roles in many disorders such as pain, drug addiction, development of tolerance to opioid drugs, and psychological disorders such as anxiety and depression. Research into the function of this receptor is an important focus of current pharmaceutical development, and selective agents such as NNC 63-0532 are essential for this work.
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MAP3K1 (or MEKK1) is a serine/threonine kinase and ubiquitin ligase that performs a pivotal role in a network of enzymes integrating cellular receptor responses to a number of mitogenic and metabolic stimuli, including: TNF receptor superfamily (TNFRs), T-cell receptor (TCR), Epidermal growth factor receptor (EGFR), and TGF beta receptor (TGFβR). Mitogen-activated protein kinase kinases (MAP2Ks) are substrates for direct phosphorylation by the MAP3K1 protein kinase. Mouse genetics has revealed that MAP3K1 is important in: embryonic development, tumorigenesis, cell growth, cell migration, cytokine production, and humoral immunity. MAP3K1 has been identified by GWAS in breast cancer.
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Human AVPR1A cDNA is 1472 bp long and encodes a 418 amino-acid long polypeptide which shares 72%, 36%, 37%, and 45% sequence identity with rat Avpr1a, human AVPR2, rat Avpr2, and human oxytocin receptor (OXTR), respectively. AVPR1A is a G-protein coupled receptor (GPCR) with 7 transmembrane domains that couples to Gaq/11 GTP binding proteins, which along with Gbl, activate phospholipase C activity. Clinically, the V1A receptor is related to vasoconstriction compared to the V1B receptor that is more related to ACTH release or the V2 receptor that is linked to the diuretic function of ADH.
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Cortisol. Note the OH at the 11 position on ring C. (The other differences between the diagrams are not of consequence.) Cortisone Cortisol, a glucocorticoid, binds the glucocorticoid receptor. However, because of its molecular similarity to aldosterone it also binds the mineralcorticoid receptor at higher concentrations. Both aldosterone and cortisol have a similar affinity for the mineralocorticoid receptor; however, there is vastly more cortisol in circulation than aldosterone. To prevent over-stimulation of the mineralocorticoid receptor by cortisol, 11β-HSD converts the biologically active cortisol to the inactive cortisone, which can no longer bind the mineralocorticoid receptor.
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Zhang et al. had previously seen that chronic cocaine administration leads to increased dendritic branching and spine density on medium spine neurons and prefrontal cortex pyramidal neurons, which may contribute to cocaine-induced neuroadaptations. When investigating the genes that were receptors and modulators, they found that expression of the sigma 1 receptor and RGS4 was not upregulated after repeat cocaine administration in DA D1 receptor mutants, suggesting functional dopamine D1 receptor is necessary for their induction. This receptor had been seen to modulate the rewarding effects of cocaine, and receptor antagonists had blocked the acute locomotor stimulating effect and lowered behavioral sensitization.
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Glutamate [NMDA] receptor subunit epsilon-2, also known as N-methyl D-aspartate receptor subtype 2B (NMDAR2B or NR2B), is a protein that in humans is encoded by the GRIN2B gene.
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Transient receptor potential cation channel subfamily M member 5 (TRPM5), also known as long transient receptor potential channel 5 is a protein that in humans is encoded by the TRPM5 gene.
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C-C chemokine receptor type 2 (CCR2 or CD192 (cluster of differentiation 192) is a protein that in humans is encoded by the CCR2 gene. CCR2 is a CC chemokine receptor.
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Eluxadoline is a μ- and κ-opioid receptor agonist and δ-opioid receptor antagonist that acts locally in the enteric nervous system, possibly decreasing adverse effects on the central nervous system.
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Melatonin receptor 1C, also known as MTNR1C, is a protein that is encoded by the Mtnr1c gene. This receptor has been identified in fish, amphibia, and birds, but not in humans.
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When the endothelial layer is disrupted, collagen and VWF anchor platelets to the subendothelium. Platelet GP1b-IX-V receptor binds with VWF; and GPVI receptor and integrin α2β1 bind with collagen.
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Hepatocyte nuclear factor 4 alpha (HNF4A) also known as NR2A1 (nuclear receptor subfamily 2, group A, member 1) is a nuclear receptor that in humans is encoded by the HNF4A gene.
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Bremelanotide is a non-selective agonist of the melanocortin receptors, MC1 through MC5 (with the exception of MC2, the receptor of ), but acting primarily as an MC3 and MC4 receptor agonist.
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Metabotropic glutamate receptor 3 (mGluR3) is an inhibitory Gi/G0-coupled G-protein coupled receptor (GPCR) generally localized to presynaptic sites of neurons. In humans, is encoded by the GRM3 gene.
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The Glycine receptor subunit alpha-3 is a protein that in humans is encoded by the GLRA3 gene. The protein encoded by this gene is a subunit of the glycine receptor.
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I2 receptor activation has also been shown to decrease body temperature, potentially mediating neuroprotective effects seen in rats. The only known antagonist for the receptor is idazoxan, which is non- selective.
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LbpAB is a receptor for human lactoferrin. TbpAB (Tbp1-Tbp2) is a receptor for human transferrin. All of these receptors are used for iron acquisition for both pathogenic and commensal species.
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The 1JC ligand is predicted to interact with the SBK3 protein (97% confidence). This ligand is functionally annotated to bind to a receptor tyrosine kinase called the hepatocyte growth factor receptor.
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Arrestins block GPCR coupling to G proteins in two ways. First, arrestin binding to the cytoplasmic face of the receptor occludes the binding site for heterotrimeric G-protein, preventing its activation (desensitization). Second, arrestin links the receptor to elements of the internalization machinery, clathrin and clathrin adaptor AP2, which promotes receptor internalization via coated pits and subsequent transport to internal compartments, called endosomes. Subsequently, the receptor could be either directed to degradation compartments (lysosomes) or recycled back to the plasma membrane where it can again signal. The strength of arrestin-receptor interaction plays a role in this choice: tighter complexes tend to increase the probability of receptor degradation (Class B), whereas more transient complexes favor recycling (Class A), although this “rule” is far from absolute.
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ISO 2720:1974 calls for reflected-light calibration to be measured by aiming the receptor at a transilluminated diffuse surface, and for incident-light calibration to be measured by aiming the receptor at a point source in a darkened room. For a perfectly diffusing test card and perfectly diffusing flat receptor, the comparison between a reflected-light measurement and an incident-light measurement is valid for any position of the light source. However, the response of a hemispherical receptor to an off-axis light source is approximately that of a cardioid rather than a cosine, so the 12% “reflectance” determined for an incident-light meter with a hemispherical receptor is valid only when the light source is on the receptor axis.
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Thus, this provided an example of how an ancestral ligand-dependent receptor could lose its ability to bind ligands. A combination of this recent evidence, as well as an in-depth study of the physical structure of the nuclear receptor ligand binding domain has led to the emergence of a new hypothesis regarding the ancestral state of the nuclear receptor. This hypothesis suggests that the ancestral receptor may act as a lipid sensor with an ability to bind, albeit rather weakly, several different hydrophobic molecules such as, retinoids, steroids, hemes, and fatty acids. With its ability to interact with a variety of compounds, this receptor, through duplications, would either lose its ability for ligand-dependent activity, or specialize into a highly specific receptor for a particular molecule.
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One category included mutants with an amino acid substitution that affected receptor recognition (since the antigenic determinant overlapped with the integrin receptor recognition site); in the other category, the substitutions affected the antigenic determinant but not the receptor recognition site. Passages of the virus in absence of the monoclonal antibody resulted in dominance of antigenic variants that maintained the receptor recognition capacity, but the dominant variants were surrounded by a cloud of mutants of the other antigenic variant category. Conversely, passages in the presence of the antibody led to selection of variants with altered receptor recognition, surrounded by a cloud of antigenic variants that maintained receptor recognition. The results underlined the role of mutant clouds in selective events, and unveiled a new mechanism of antigenic flexibility.
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P2Y12 antagonists and how they bind to the receptor.
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COX5B has been shown to interact with Androgen receptor.
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D2 receptor signaling may mediate protein kinase B, arrestin beta 2, and GSK-3 activity, and inhibition of these proteins results in stunting of the hyperlocomotion in amphetamine treated rats. Dopamine receptors can also transactivate Receptor tyrosine kinases.name="receptor mechanism" Beta Arrestin recruitment is mediated by G-protein kinases that phosphorylate and inactivate dopamine receptors after stimulation. While beta arrestin plays a role in receptor desensitization, it may also be critical in mediating downstream effects of dopamine receptors.
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Tesevatinib (KD019, XL647) is an experimental drug proposed for use in kidney cancer and polycystic kidney disease. The drug was first developed by Exelixis, Inc. and was later acquired by Kadmon Corporation. Tesevatinib binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including epidermal growth factor receptor (EGFR; ERBB1), epidermal growth factor receptor 2 (HER2; ERBB2), vascular endothelial growth factor receptor (VEGFR), and ephrin B4 (EphB4).
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G protein coupled receptor 132, also termed G2A, is classified as a member of the proton sensing G protein coupled receptor (GPR) subfamily. Like other members of this subfamily, i.e. GPR4, OGR1 (GPR68), and TDAG8 (GPR65), G2A is a G protein coupled receptor that resides in the cell surface membrane, senses changes in extracellular pH, and can alter cellular function as a consequence of these changes. Subsequently, G2A was suggested to be a receptor for lysophosphatidylcholine (LPC).
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C-C chemokine receptor type 11 is a protein that in humans is encoded by the CCRL1 gene. The protein encoded by this gene is a member of the G protein- coupled receptor family, and is a receptor for C-C type chemokines. This receptor has been shown to bind dendritic cell- and T cell-activated chemokines including CCL19/ELC, CCL21/SLC, and CCL25/TECK. Alternatively spliced transcript variants encoding the same protein have been described.
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Interleukin 36, or IL-36, is a group of cytokines in the IL-1 family with pro- inflammatory effects. The role of IL-36 in inflammatory diseases is under investigation. There are four members of the IL-36 family which bind to the IL-36 receptor (IL1RL2/IL-1Rrp2/IL-36 receptor dimer) with varying affinities. IL36A, IL36B, and IL36G are IL-36 receptor agonists. IL36RA is an IL-36 receptor antagonist, inhibiting IL-36R signaling.
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Wnt signaling begins when a Wnt protein binds to the N-terminal extra-cellular cysteine-rich domain of a Frizzled (Fz) family receptor. These receptors span the plasma membrane seven times and constitute a distinct family of G-protein coupled receptors (GPCRs). However, to facilitate Wnt signaling, co-receptors may be required alongside the interaction between the Wnt protein and Fz receptor. Examples include lipoprotein receptor-related protein (LRP)-5/6, receptor tyrosine kinase (RTK), and ROR2.
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Estrogen esters are essentially inactive themselves, with esters such as estradiol valerate and estradiol sulfate having about 2% of the affinity of estradiol for the estrogen receptor. Likewise, the estrogen ether mestranol (ethinylestradiol 3-methyl ether) has about 1% of the affinity of estradiol for the estrogen receptor. Estrone sulfate has less than 1% of the affinity of estradiol for the estrogen receptor. As such, estrogen esters do not bind to the estrogen receptor except at extremely high concentrations.
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The human V3 receptor (V3R, previously known as V1BR) is a G-protein-coupled pituitary receptor that, because of its scarcity, was only recently characterized. The 424-amino-acid sequence of the V3R has homologies of 45%, 39%, and 45% with the V1R, V2R and oxytocin receptor (OTR), respectively. However, V3R has a pharmacologic profile that distinguishes it from the human V1R and activates several signaling pathways via different G-proteins, depending on the level of receptor expression.
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Quinupramine (brand names Kevopril, Kinupril, Adeprim, Quinuprine) is a tricyclic antidepressant (TCA) used in Europe for the treatment of depression. Pharmacologically, quinupramine acts in vitro as a strong muscarinic acetylcholine receptor antagonist (anticholinergic) and H1 receptor antagonist (antihistamine), moderate 5-HT2 receptor antagonist, and weak serotonin and norepinephrine reuptake inhibitor. It has negligible affinity for the α1-adrenergic, α2-adrenergic, β-adrenergic, or D2 receptor. Clinically, quinupramine is reported to be stimulating similarly to imipramine, desipramine, and demexiptiline.
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The apochromodulin is stored in insulin sensitive cells in the nucleus. When blood glucose levels rise, insulin is released into the bloodstream and binds to an external α-subunit of the insulin receptor, a transmembrane protein. The insulin receptor consists of 2 extracellular α-subunits and 2 transmembrane β-subunits. As soon as insulin binds to the insulin receptor, a conformational change in the receptor occurs, causing all 3 tyrosine residues (located in the β-subunits) to be phosphorylated.
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Enciprazine (INN, BAN; enciprazine hydrochloride (USAN); developmental code names WY-48624, D-3112), is an anxiolytic and antipsychotic of the phenylpiperazine class which was never marketed. It shows high affinity for the α1-adrenergic receptor and 5-HT1A receptor, among other sites. The drug was initially anticipated to produce ortho-methoxyphenylpiperazine (oMeOPP), a serotonin receptor agonist with high affinity for the 5-HT1A receptor, as a significant active metabolite, but subsequent research found this not to be the case.
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Mineralocorticoids bind to the mineralocorticoid receptor in the cell cytosol, and are able to freely cross the lipid bilayer of the cell. This type of receptor becomes activated upon ligand binding. After a hormone binds to the corresponding receptor, the newly formed receptor-ligand complex translocates into the cell nucleus, where it binds to many hormone response elements (HREs) in the promoter region of the target genes in the DNA. The opposite mechanism is called transrepression.
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The mature IGF-1R has a molecular weight of approximately 320 kDa.citation? The receptor is a member of a family which consists of the insulin receptor and the IGF-2R (and their respective ligands IGF-1 and IGF-2), along with several IGF-binding proteins. IGF-1R and the insulin receptor both have a binding site for ATP, which is used to provide the phosphates for autophosphorylation. There is a 60% homology between IGF-1R and the insulin receptor.
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Mutations in this receptor cause familial glucocorticoid deficiency (FGD) type 1, in which patients have high levels of serum ACTH and low levels of cortisol. Mutation of the receptor gene causes 25% of FGD, and mutation on the MRAP gene causes 20% of FGD. Mutations of ACTH can also contribute to this pathology: mutation of the "message sequence" inhibits cAMP production when bound to the ACTH receptor, and mutation of the "address sequence" inhibits binding to the receptor altogether.
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Many co-receptor-related disorders occur due to mutations in the receptor's coding gene. LRP5 (low- density lipoprotein receptor-related protein 5) acts as a co-receptor for the Wnt-family of glycoproteins which regulate bone mass. Malfunctions in this co- receptor lead to lower bone density and strength which contribute to osteoporosis.Sawakami, K., Robling, A.G., Ai, M., Pitner, N.D., Liu, D., Warden, S.J., Li, J., Maye, P., Rowe, D.W., Duncan, R.L., Warman, M.L., Turner, C.H. (2006).
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This "classical" PTH receptor is expressed in high levels in bone and kidney and regulates calcium ion homeostasis through activation of adenylate cyclase and phospholipase C. In bone, it is expressed on the surface of osteoblasts. When the receptor is activated through PTH binding, osteoblasts express RANKL (Receptor Activator of Nuclear Factor kB Ligand), which binds to RANK (Receptor Activator of Nuclear Factor kB) on osteoclasts. This turns on osteoclasts to ultimately increase the resorption rate.
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The encoded protein is a single pass type I membrane protein and acts as the receptor for colony stimulating factor 1, a cytokine which controls the production, differentiation, and function of macrophages. This receptor mediates most, if not all, of the biological effects of this cytokine. Ligand binding activates CSF1R through a process of oligomerization and trans-phosphorylation. The encoded protein is a tyrosine kinase transmembrane receptor and member of the CSF1/PDGF receptor family of tyrosine-protein kinases.
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The PEPR1 and PEPR2 kinases that bind to the receptors AtPEPR1 and AtPEPR2, respectively were identified. Through photolabeling with a radioactively marked ligand, an AtPep1 receptor was able to be purified and later duplicated. This led to the discovery of the first damage associated molecular pattern or DAMP/pattern recognition receptor couple in Arabidopsis, otherwise known as the thale cress, which is a small flowering plant common in Eurasia. This discovered receptor was coined PEPR1, PEP receptor 1.
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Low-density lipoprotein receptor-related protein 8 (LRP8), also known as apolipoprotein E receptor 2 (ApoER2), is a protein that in humans is encoded by the LRP8 gene. ApoER2 is a cell surface receptor that is part of the low- density lipoprotein receptor family. These receptors function in signal transduction and endocytosis of specific ligands. Through interactions with one of its ligands, reelin, ApoER2 plays an important role in embryonic neuronal migration and postnatal long-term potentiation.
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The dopamine receptor D4 is a dopamine D2-like G protein-coupled receptor encoded by the gene on chromosome 11 at 11p15.5. The structure of DRD4 was recently reported in complex with the antipsychotic drug nemonapride. As with other dopamine receptor subtypes, the D4 receptor is activated by the neurotransmitter dopamine. It is linked to many neurological and psychiatric conditions including schizophrenia and bipolar disorder, ADHD, addictive behaviors, Parkinson's disease, and eating disorders such as anorexia nervosa.
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BD1008 or N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-1-pyrrolidineethanamine is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1008 significantly attenuates the behavioral toxicity of cocaine, and may be potentially useful in the development of antidotes for the treatment of cocaine overdose.
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Metabolic regulation of glycogen by glucagon. Glucagon binds to the glucagon receptor, a G protein-coupled receptor, located in the plasma membrane of the cell. The conformation change in the receptor activates G proteins, a heterotrimeric protein with α, β, and γ subunits. When the G protein interacts with the receptor, it undergoes a conformational change that results in the replacement of the GDP molecule that was bound to the α subunit with a GTP molecule.
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Myristoylation is an integral part of apoptosis, or programmed cell death. Apoptosis is necessary for cell homeostasis and occurs when cells are under stress such as hypoxia or DNA damage. Apoptosis can proceed by either mitochondrial or receptor mediated activation. In receptor mediated apoptosis, apoptotic pathways are triggered when the cell binds a death receptor.
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Epidermal growth factor receptor kinase substrate 8-like protein 2 is an enzyme that in humans is encoded by the EPS8L2 gene. This gene encodes a protein that is related to epidermal growth factor receptor pathway substrate 8 (EPS8), a substrate for the epidermal growth factor receptor. The function of this protein is unknown.
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A third classification of receptors is by how the receptor transduces stimuli into membrane potential changes. Stimuli are of three general types. Some stimuli are ions and macromolecules that affect transmembrane receptor proteins when these chemicals diffuse across the cell membrane. Some stimuli are physical variations in the environment that affect receptor cell membrane potentials.
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G-protein-coupled receptor oligomerisation is a widespread phenomenon. One of the best-studied examples is the metabotropic GABAB receptor. This so-called constitutive receptor is formed by heterodimerization of GABABR1 and GABABR2 subunits. Expression of the GABABR1 without the GABABR2 in heterologous systems leads to retention of the subunit in the endoplasmic reticulum.
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The GFRA2 protein is a glycosylphosphatidylinositol(GPI)-linked cell surface receptor. It is part of the GDNF receptor family. Glial cell line-derived neurotrophic factor (GDNF) and neurturin (NTN) are two structurally related, potent neurotrophic factors that play key roles in the control of neuron survival and differentiation. They both bind the GFRA2 receptor.
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Efficacy spectrum of receptor ligands. In the field of pharmacology, a superagonist is a type of agonist that is capable of producing a maximal response greater than the endogenous agonist for the target receptor, and thus has an efficacy of more than 100%. For example, goserelin is a superagonist of the gonadotropin-releasing hormone receptor.
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G-protein-coupled receptor kinase 3 (GRK3) is an enzyme that in humans is encoded by the ADRBK2 gene. GRK3 was initially called Beta-adrenergic receptor kinase 2 (βARK-2), and is a member of the G protein-coupled receptor kinase subfamily of the Ser/Thr protein kinases that is most highly similar to GRK2.
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Hypoprolactinemia can result from autoimmune disease, hypopituitarism, growth hormone deficiency, hypothyroidism, excessive dopamine action in the tuberoinfundibular pathway and/or the anterior pituitary, and ingestion of drugs that activate the D2 receptor, such as direct D2 receptor agonists like bromocriptine and pergolide, and indirect D2 receptor activators like amphetamines (through the induction of dopamine release).
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It requires BMP signaling for its expression FKBP12 binds the GS region of the type I receptor preventing phosphorylation of the receptor by the type II receptors. It is believed that FKBP12 and its homologs help to prevent type I receptor activation in the absence of a ligands, since ligand binding causes its dissociation.
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Part of this signaling may be via IGF1R/insulin receptor heterodimers (the reason for the confusion is that binding studies show that IGF1 binds the insulin receptor 100-fold less well than insulin, yet that does not correlate with the actual potency of IGF1 in vivo at inducing phosphorylation of the insulin receptor, and hypoglycemia).
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DOB is a 5-HT2A, 5-HT2B, and 5-HT2C receptor agonist or partial agonist. Its psychedelic effects are mediated by its agonistic properties at the 5-HT2A receptor. Due to its selectivity, DOB is often used in scientific research when studying the 5-HT2 receptor subfamily. It is an agonist of human TAAR1.
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The mechanism of action of SEP-363856 in the treatment of schizophrenia is unclear. However, it is thought to be an agonist at the trace amine-associated receptor 1 (TAAR1) and serotonin-1A receptor (5-HT1A) receptors. This mechanism of action is unique among available antipsychotics, which generally antagonize dopamine receptors (especially dopamine receptor D2).
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The DAF-7 gene encodes for the ortholog of GDF11, a ligand of TGF-beta signaling pathway, in the worm Caenorhabditis elegans. When binds to the complex of type II receptor Daf-4 and type I receptor Daf-1, this receptor protein serine/threonine kinase will phosphorylation activate the Smad Protein Daf-8/14.
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Types of Chemosensors. (1.) Indicator- spacer-receptor (ISR) (2.) Indicator-Displacement Assay (IDA) IDA offers several advantages versus the traditional ISR chemical sensing approach. First, it does not require the indicator to be covalently bound to the receptor. Secondly, since there is no covalent bond, various indicators can be used with the same receptor.
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Complement receptor type 2 (CR2), also known as complement C3d receptor, Epstein-Barr virus receptor, and CD21 (cluster of differentiation 21), is a protein that in humans is encoded by the CR2 gene. CR2 is involved in the complement system. It binds to iC3b (inactive derivative of C3b), C3dg, or C3d.Frank K, Atkinson JP (2001).
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The bound antagonists may prevent conformational changes in the receptor required for receptor activation after the agonist binds.D.E. Golan, A.H Tashjian Jr, E.J. Armstrong, A.W. Armstrong. (2007) Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy Lippincott Williams & Wilkins Cyclothiazide has been shown to act as a reversible non-competitive antagonist of mGluR1 receptor.
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The angiotensin receptor is activated by the vasoconstricting peptide angiotensin II. The activated receptor in turn couples to Gq/11 and thus activates phospholipase C and increases the cytosolic Ca2+ concentrations, which in turn triggers cellular responses such as stimulation of protein kinase C. Activated receptor also inhibits adenylate cyclase and activates various tyrosine kinases.
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This gene and the gene encoding the colony stimulating factor 2 receptor alpha chain (CSF2RA) form a cytokine receptor gene cluster in a X-Y pseudoautosomal region on chromosomes X or Y.
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In the adrenal medulla, acetylcholine is used as a neurotransmitter, and the receptor is of the nicotinic type. The somatic nervous system uses a nicotinic receptor to acetylcholine at the neuromuscular junction.
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Angiopoietin-1 receptor also known as CD202B (cluster of differentiation 202B) is a protein that in humans is encoded by the TEK gene. Also known as TIE2, it is an angiopoietin receptor.
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Sphingosine-1-phosphate receptor 2 also known as S1PR2 or S1P2 is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P).
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The gene expression of these isoenzymes is regulated by human pregnane receptor X (PXR) and constitutive androstane receptor (CAR). Phenobarbital induction of CYP2B6 is mediated by both. Primidone does not activate PXR.
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Cyclopropane is inactive at the GABAA and glycine receptors, and instead acts as an NMDA receptor antagonist. It also inhibits the AMPA receptor and nicotinic acetylcholine receptors, and activates certain K2P channels.
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Spiramide (developmental code name AMI-193) is an experimental antipsychotic that acts as a selective 5-HT2A, 5-HT1A, and D2 receptor antagonist. It has negligible affinity for the 5-HT2C receptor.
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Guanfacine is a highly selective agonist of the α2A adrenergic receptor, with low affinity for other receptors. However, it may also be a potent 5-HT2B receptor agonist, potentially contributing to valvulopathy.
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Receptor expression-enhancing protein 5 is a protein that in humans is encoded by the REEP5 gene. Receptor Expression Enhancing Protein is a protein encoded for in Humans by the REEP5 gene.
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Anionic nanoparticles are primarily taken up by these zebrafish SECs by the scavenger receptor, stabilin-2 in this process, which is also a signature scavenger receptor of mammalian liver sinusoidal endothelial cells.
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The action of calcitriol is mediated by the vitamin D receptor, a nuclear receptor which regulates the synthesis of hundreds of proteins and is present in virtually every cell in the body.
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This produces α-muricholic acid from chenodeoxycholic acid, and β-muricholic acid from ursodeoxycholic acid. Tauromuricholic acids were shown to be potent antagonists of the bile acid receptor farnesoid X receptor (FXR).
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The mechanism of action of cimetidine as an antacid is as a histamine H2 receptor antagonist. It has been found to bind to the H2 receptor with a Kd of 42 nM.
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Pituitary adenylate cyclase-activating polypeptide type I receptor also known as PAC1, is a protein that in humans is encoded by the ADCYAP1R1 gene. This receptor binds pituitary adenylate cyclase activating peptide.
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A selective PPAR modulator (SPPARM) is a selective receptor modulator of the peroxisome proliferator-activated receptor (PPAR). Examples include SPPARMs of the PPARγ, BADGE, EPI-001, INT-131, MK-0533, and S26948.
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Probable ATP-dependent RNA helicase DHX58 also known as RIG-I-like receptor 3 (RLR-3) or RIG-I-like receptor LGP2 (RLR) is a RIG-I-like receptor dsRNA helicase enzyme that in humans is encoded by the DHX58 gene. The protein encoded by the gene DHX58 is known as LGP2 (Laboratory of Genetics and Physiology 2).
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The angiotensin receptor is activated by the vasoconstricting peptide angiotensin II. The activated receptor in turn couples to Gq/11 and Gi/o and thus activates phospholipase C and increases the cytosolic Ca2+ concentrations, which in turn triggers cellular responses such as stimulation of protein kinase C. Activated receptor also inhibits adenylate cyclase and activates various tyrosine kinases.
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G-protein-coupled receptor kinase 2 (GRK2) is an enzyme that in humans is encoded by the ADRBK1 gene. GRK2 was initially called Beta-adrenergic receptor kinase (βARK or βARK1), and is a member of the G protein-coupled receptor kinase subfamily of the Ser/Thr protein kinases that is most highly similar to GRK3(βARK2).
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D5 receptor is highly homologous to the D1 receptor. Their amino acid sequences are 49% to 80% identical. D5 receptor has a long C-terminus of 93 amino acids, accounting for 26% of the entire protein. In spite of the high degree of homology between D5 and D1 receptors, their c-terminus tails have little similarity.
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Few highly selective ligands are commercially available for the 5-HT5A receptor. When selective activation of this receptor is desired in scientific research, the non-selective serotonin receptor agonist 5-Carboxamidotryptamine can be used in conjunction with selective antagonists for its other targets (principally 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT7). Research in this area is ongoing.
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For example, 5-HT1E receptors are abundant in the hippocampus but are not detectable in the striatum (caudate and putamen of the human brain), while the opposite is true for the 5-HT1F receptor. Thus, conclusions about the function of the 5-HT1E receptor cannot be ascribed to the function of the 5-HT1F receptor, and vice versa.
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They may have various functions within the cell: catalysis of chemical reactions (enzyme- substrate), defense of the organism through the immune system (antibodies antigen complexes), signal transduction (receptor-ligand complexes) that consists of a transmembrane receptor that upon binding the ligand activates an intracellular cascade. Lipophilic hormonal receptor complexes can pass the nuclear membrane where transcription may be regulated.
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Ifenprodil is an inhibitor of the NMDA receptor, specifically of GluN1 (glycine-binding NMDA receptor subunit 1) and GluN2B (glutamate-binding NMDA receptor subunit 2) subunits. Additionally, ifenprodil inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors. NMDA receptors are multimeric ionotropic glutamate receptors composed of four subunits. GluN1 is obligate for functional expression.
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The signal sequence receptor (SSR) is a glycosylated endoplasmic reticulum (ER) membrane receptor associated with protein translocation across the ER membrane. The SSR consists of 2 subunits, a 34-kD glycoprotein (alpha-SSR or SSR1) and a 22-kD glycoprotein (beta-SSR or SSR2). The human beta-signal sequence receptor gene (SSR2) maps to chromosome bands 1q21-q23.
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NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor. The new finding has raised significant concerns about studies using NAN-190 as a specific serotonin receptor antagonist.
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The secretion of parathyroid hormone (PTH) is regulated by the interaction of the calcium-sensing receptor with calcium in the blood. The calcium-sensing receptor is present on the plasma membrane of the chief cells. The CaR is a G protein-coupled receptor, as part of the C family. The CaR is divided into three general domains.
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It is monomeric and binds one IgE molecule. The α chain binds IgE and the other three chains contain immune receptor tyrosine-based activation motifs (ITAM). Then oligomeric antigens bind to receptor-bound IgE to crosslink two or more of these receptors. This crosslinking then recruits doubly acylated non- receptor Src-like tyrosine kinase Lyn to phosphorylate ITAMs.
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SARA orients the R-SMAD such that serine residue on its C-terminus faces the catalytic region of the Type I receptor. The Type I receptor phosphorylates the serine residue of the R-SMAD. Phosphorylation induces a conformational change in the MH2 domain of the R-SMAD and its subsequent dissociation from the receptor complex and SARA.
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Adaptor proteins TRAF2 and TRAF5 have been shown to mediate the signaling process of this receptor. CD27-binding protein (SIVA), a proapoptotic protein, can bind to this receptor and is thought to play an important role in the apoptosis induced by this receptor. In murine γδ T cells its expression has been correlated with the secretion of IFNγ.
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Figure 5. Putative binding of aplaviroc to the CCR5 receptor Figure 6. Putative binding of maraviroc to the CCR5 receptor CCR5 is a member of G protein-coupled, seven transmembrane segment receptors. The structure of the receptor comprises seven-helix bundle in the transmembrane region, these regions are labeled I–VII in figures 5 and 6.
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Figure 1. The seven transmembrane α-helix structure of a G-protein-coupled receptor. A neurotransmitter receptor (also known as a neuroreceptor) is a membrane receptor protein that is activated by a neurotransmitter. Chemicals on the outside of the cell, such as a neurotransmitter, can bump into the cell's membrane and along the membrane we can find receptors.
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LY-266,097 is a research ligand which acts as a potent and selective antagonist for the 5-HT2B receptor, with more than 100x selectivity over the related 5-HT2A and 5-HT2C receptor subtypes.McCorvy JD, Wacker D, Wang S, et al. Structural determinants of 5-HT2B receptor activation and biased agonism. Nat Struct Mol Biol. 2018;25(9):787-796.
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A smaller class of 3FTx proteins binds instead to muscarinic acetylcholine receptors, a family of G-protein-coupled receptors. Muscarinic toxins can be either receptor agonists or receptor antagonists, and in some cases the same 3FTx protein is an agonist at one receptor subtype and an antagonist at another. Muscarinic toxins are generally of the short-chain type.
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" Journal of Cytology/Indian Academy of Cytologists 31.2 (2014): 96. Cytologically, the cells of apocrine carcinoma are relatively large, granular, and it has a prominent eosinophilic cytoplasm. (accessed November 3, 2014) When apocrine carcinoma is tested as a “triple negative", it means that the cells of the patient cannot express the estrogen receptor, progesterone receptor, or HER2 receptor.
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It has been used in China since the 1970s. Anordrin has both weak estrogenic and antiestrogenic activity. It binds to the estrogen receptor but does not bind to the androgen receptor or the progesterone receptor. In animals, anordrin has antigonadotropic effects, and in male animals, inhibits spermatogenesis and causes atrophy of the epididymis, prostate, and seminal vesicles.
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The oxytocin receptor, also known as OXTR, is a protein which functions as receptor for the hormone and neurotransmitter oxytocin. In humans, the oxytocin receptor is encoded by the OXTR gene which has been localized to human chromosome 3p25. Evolutionary tree of the oxytocin, vasotocin, mesotocin and isotocin receptors and their ligands. From Koechbach et al.
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Both are believed to mediate antiproliferative effects. Functional interactions with the EGF receptor and the type I/type II TGFβ receptor system have also been reported, and other cell-surface proteins such as proteoglycans also bind IGFBP-3. IGFBP-3 can enter cells by both clathrin-mediated and caveolin- mediated endocytosis. possibly involving the transferrin receptor.
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Transferrin receptor (TfR) is a carrier protein for transferrin. It is needed for the import of iron into the cell and is regulated in response to intracellular iron concentration. It imports iron by internalizing the transferrin-iron complex through receptor-mediated endocytosis.; Figure 3: The cycle of transferrin and transferrin receptor 1-mediated cellular iron uptake.
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The muscarinic acetylcholine receptor, also known as cholinergic/acetylcholine receptor M3, or the muscarinic 3, is a muscarinic acetylcholine receptor encoded by the human gene CHRM3. The M3 muscarinic receptors are located at many places in the body, e.g., smooth muscles, the endocrine glands, the exocrine glands, lungs, pancreas and the brain. In the CNS, they induce emesis.
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Fig 4. Schematic picture of sumatriptan binding to 5-HT1D receptor A schematic drawing of the binding of sumatriptan to 5-HT1D receptor can be seen in figure 4. One study showed that sumatriptan fits better in the binding site of the receptor when the side chain with the protonated nitrogen atom is folded back over the indole structure.
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Metabotropic glutamate receptor 2 (mGluR2) is a protein that, in humans, is encoded by the GRM2 gene. mGluR2 is a G protein-coupled receptor (GPCR) that couples with the Gi alpha subunit. The receptor functions as an autoreceptor for glutamate, that upon activation, inhibits the emptying of vesicular contents at the presynaptic terminal of glutamatergic neurons.
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The protein encoded by this gene is a member of the TNF-receptor superfamily. The cytoplasmic region of this receptor was found to bind to several TNF receptor associated factor (TRAF) family members, which may mediate the signal transduction pathways that activate the immune response. In melanocytic cells TNFRSF14 gene expression may be regulated by MITF.
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Several ion channels and neurotransmitters receptors pre-mRNa are substrates for ADARs. This includes 5 subunits of the glutamate receptor ionotropic AMPA glutamate receptor subunits (Glur2, Glur3, Glur4) and Kainate receptor subunits (Glur5, Glur6). Glutamate-gated ion channels are made up of four subunits per channel. Their function is in the mediation of fast neurotransmission to the brain.
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It is an accessory chain essential for the active interleukin 10 receptor complex. Coexpression of this and IL10RA proteins has been shown to be required for IL10-induced signal transduction. This gene and three other interferon receptor genes, IFNAR2, IFNAR1, and IFNGR2, form a class II cytokine receptor gene cluster located in a small region on chromosome 21.
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Cicutoxin binds to the same place as GABA, because of this the receptor is not activated by GABA. The pore of the receptor won't open and chloride can't flow across the membrane. Binding of cicutoxin to the beta domain also blocks the chloride channel. Both effects of cicutoxin on the GABAA-receptor cause a constant depolarization.
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Interleukin 12 receptor, beta 2 subunit is a subunit of the interleukin 12 receptor. IL12RB2 is its human gene. IL12RB2 orthologs have been identified in all mammals for which complete genome data are available. The protein encoded by this gene is a type I transmembrane protein identified as a subunit of the interleukin 12 receptor complex.
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The granulocyte-macrophage colony-stimulating factor receptor also known as CD116 (Cluster of Differentiation 116), is a receptor for granulocyte- macrophage colony-stimulating factor, which stimulates the production of white blood cells. The receptor is normally located on myeloblast, mature neutrophil, but not on any erythroid or megakaryocytic lineage cells. It is associated with Surfactant metabolism dysfunction type 4.
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Receptor protein serine/threonine kinases () are enzyme-linked receptors that belong to protein-serine/threonine kinases. The systematic name of this enzyme class is ATP:[receptor-protein] phosphotransferase. Proteins from this group participate in 7 metabolic pathways: MAPK signaling pathway, cytokine-cytokine receptor interaction, TGF beta signaling pathway, adherens junction, colorectal cancer, pancreatic cancer, and chronic myeloid leukemia.
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"Methods for treating sleep disorders by cholecystokinin (CCK) receptor B antagonists": Inventors: David W. Carley and Miodrag Radulovacki. # "Pharmacological treatments for sleep disorders (apnoe) with prostanoid receptor antagonists", Inventors: David W. Carley and Miodrag Radulovacki, US Patent 8,076,315, Dec. 13, 2011."Pharmacological treatments for sleep disorders (apnoe) with prostanoid receptor antagonists": Inventors: David W. Carley and Miodrag Radulovacki.
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17α-OHP is an agonist of the progesterone receptor (PR) similarly to progesterone, albeit weakly in comparison. In addition, it is an antagonist of the mineralocorticoid receptor (MR) as well as a partial agonist of the glucocorticoid receptor (GR), albeit with very low potency (EC50 >100-fold less relative to cortisol) at the latter site, also similarly to progesterone.
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Each G protein is a heterotrimer of three subunits: α-, β-, and γ- subunits. The α-subunit (Gα) typically binds the G protein to a transmembrane receptor protein known as a G protein-coupled receptor, or GPCR. This receptor protein has a large, extracellular binding domain which will bind its respective ligands (e.g. neurotransmitters and hormones).
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Decoy receptors, or sink receptors, are receptors that bind a ligand, inhibiting it from binding to its normal receptor. For instance, the receptor VEGFR-1 can prevent vascular endothelial growth factor (VEGF) from binding to the VEGFR-2 The TNF inhibitor etanercept exerts its anti-inflammatory effect by being a decoy receptor that binds to TNF.
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Specifically, quizartinib selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs). Mutations cause constant activation of the FLT3 pathway resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis.
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T cells recognise antigens primarily via the T cell receptor. This receptor needs various co-receptors to function, one of which is CD3. The T cell receptor-CD3 complex transduces the signal for the T cell to proliferate and attack the antigen. Muromonab-CD3 is a murine (mouse) monoclonal IgG2a antibody which was created using hybridoma technology.
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Heteromerization of 2 and D5 receptors can be disrupted through changes of single amino acids in the c-terminus of the D5 receptor. Dopamine receptor D5 has been shown to interact with GABRG2.
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MLGA is a progestogen, and hence is an agonist of the progesterone receptor. It has been found to possess 73% of the affinity of progesterone for the progesterone receptor in rhesus monkey uterus.
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However, the roles of G2A as a pH-sensor or LPC receptor are disputed. Rather, current studies suggest that it is a receptor for certain metabolites of the polyunsaturated fatty acid, linoleic acid.
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Fc receptor-like protein 4 is a protein that in humans is encoded by the FCRL4 gene. FCRL4 is an inhibitory receptor expressed on human memory B cells which resides in epithelial tissues.
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A glycinergic agent (or drug) is a chemical which functions to directly modulate the glycine system in the body or brain. Examples include glycine receptor agonists, glycine receptor antagonists, and glycine reuptake inhibitors.
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G protein-coupled receptor 137B also known as GPR137B is a G protein-coupled receptor which in humans is encoded by the GPR137B gene. The expression of GPR137B is upregulated during kidney development.
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G protein-coupled receptor 148, also known as GPR148, is a human orphan receptor from GPCR superfamily. It is expressed primarily in nervous system and testis. Is may be implicated in prostate cancer.
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SB-204070 is a drug which acts as a potent and selective 5-HT4 serotonin receptor antagonist (or weak partial agonist), and is used for research into the function of this receptor subtype.
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One effect of this receptor is to activate deiodinases which convert the prohormone thyroxine (T4) to the active hormone triiodothyronine (T3). T3 in turn activates the thyroid hormone receptor which increases metabolic rate.
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Gamma-aminobutyric acid receptor subunit rho-3 is a protein that in humans is encoded by the GABRR3 gene. The protein encoded by this gene is a subunit of the GABAA-ρ receptor.
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C-C chemokine receptor-like 2 is a protein that in humans is encoded by the CCRL2 gene. Recently it was found that CCRL2 also acts as a receptor for the chemokine chemerin.
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The use of a snake venom toxin to characterize the cholinergic receptor protein. Proc. Natl. Acad. Sci. USA 67: 1241-1247. The isolation of the receptor was also later reported by Ricardo Miledi.
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The clinical implications of this receptor have not been fully explored; however, stimulation of this receptor is known to effectively decrease cyclic AMP levels and downregulate the activity of protein kinase A (PKA).
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81 7328-32 1984. His final work was directed toward isolation of the ACTH receptor using the same approach used on the insulin receptor but by this time his health was in decline.
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DNAJC14 has been shown to interact with Dopamine receptor D1.
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A complex of amnionless and cubilin forms the cubam receptor.
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CLIC6 has been shown to interact with Dopamine receptor D3.
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Many selective ligands for the CB2 receptor are now available.
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RNF12 has been shown to interact with Estrogen receptor alpha.
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POU4F2 has been shown to interact with Estrogen receptor alpha.
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RNF14 has been shown to interact with the Androgen receptor.
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Blocking this receptor leads to smooth muscle relaxation and vasodilation.
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The receptor defect is an autosomal recessive mutation or polymorphism.
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DNTTIP2 has been shown to interact with Estrogen receptor alpha.
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This protein may play a role as a scavenger receptor.
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The cholecystokinin B receptor responds to a number of ligands.
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XBP1 has been shown to interact with estrogen receptor alpha.
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Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor.
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ISL1 has been shown to interact with Estrogen receptor alpha.
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Isoguvacine is a GABAA receptor agonist used in scientific research.
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SGTA has been shown to interact with Growth hormone receptor.
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GPR17 has a structure which is intermediate between the cysteinyl leukotriene receptor group (i.e. cysteinyl leukotriene receptor 1 and cysteinyl leukotriene receptor 2) and the purine P2Y subfamily of 12 receptors (see P2Y receptors), sharing 28 to 48% amino acid identity with them. GPR17 is a G protein coupled receptor that acts primarily through G proteins linked to the Gi alpha subunit but also to Gq alpha subunit. Matching these structural relationships, GPR17 has been reported to be activated by cysteinyl leukotrienes (i.e.
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Azapirones such as buspirone, gepirone, and tandospirone are 5-HT1A receptor partial agonists marketed primarily as anxiolytics, but also as antidepressants. The antidepressants vilazodone and vortioxetine are 5-HT1A receptor partial agonists. Flibanserin, a drug used for female sexual dysfunction, is a 5-HT1A receptor partial agonist. Many atypical antipsychotics, such as aripiprazole, asenapine, clozapine, lurasidone, quetiapine, and ziprasidone, are 5-HT1A receptor partial agonists, and this action is thought to contribute to their beneficial effects on negative symptoms in schizophrenia.
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The GLP2 receptor (GLP2R) is a G protein-coupled receptor superfamily member closely related to the glucagon receptor (GLP1 receptor). Glucagon-like peptide-2 (GLP2) is a 33-amino acid proglucagon-derived peptide produced by intestinal enteroendocrine cells. Like glucagon-like peptide-1 (GLP1) and glucagon itself, it is derived from the proglucagon peptide encoded by the GCG gene. GLP2 stimulates intestinal growth and upregulates villus height in the small intestine, concomitant with increased crypt cell proliferation and decreased enterocyte apoptosis.
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This receptor is a glycosylated, 7-transmembrane G-protein coupled receptor that activates the phospholipase C signaling pathway. The receptor is aberrantly expressed in numerous cancers such as those of the lung, colon, and prostate. An individual with autism and multiple exostoses was found to have a balanced translocation between chromosome 8 and a chromosome X breakpoint located within the gastrin-releasing peptide receptor gene. The transcription factor CREB is a regulator of human GRP-R expression in colon cancer.
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Some allosteric modulators induce a conformational change in their target receptor which increases the binding affinity and/or efficacy of the receptor agonist. Examples of such modulators include benzodiazepines and barbiturates, which are GABAA receptor positive allosteric modulators. Benzodiazepines like diazepam bind between α and γ subunits of the GABAA receptor ion channels and increase the channel opening frequency, but not the duration of each opening. Barbiturates like phenobarbital bind β domains and increase the duration of each opening, but not the frequency.
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Most of the candidate receptor genes are in clusters of similar genes; 11 of these appear to be expressed in small subsets of chemosensory neurons. A single type of neuron can potentially express at least 4 different receptor genes. Some of these might encode receptors for water-soluble attractants, repellents and pheromones, which are divergent members of the G-protein-coupled receptor family. Sequences of the Sra family of C. elegans receptor-like proteins contain 6-7 hydrophobic, putative transmembrane, regions.
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In 1991, the phenomenon of receptor crosstalk was observed between adenosine A2A (A2A) and dopamine D2 receptor (DRD2) thus suggesting the formation of heteromers. While initially thought to be a receptor heterodimer, a review from 2015 determined that the A2A-DRD2 heteromer is a heterotetramer composed of A2A and DRD2 homodimers (i.e., two adenosine A2A receptors and two dopamine D2 receptors). Maggio and co-workers showed in 1993 the ability of the muscarinic M3 receptor and α2C-adrenoceptor to heterodimerize.
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Once the receptor and PA returns to the lipid raft, E3 ubiquitin ligase Cb1 ubiquitinates the cytoplasmic tail of the receptor, signaling the receptor and associated toxin proteins for endocytosis. Dynamin and Eps15 are required for this endocytosis to occur, indicating that anthrax toxin enters the cell via the clathrin-dependent pathway.Abrami, L.; Liu, S.; Cosson, P.; Leppla, S. H.; van der Goot, F. G. Anthrax toxin triggers endocytosis of its receptor via a lipid raft-mediated clathrin-dependent process. J. Cell Biol.
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The B2 receptor is a G protein-coupled receptor, coupled to Gq and Gi. Gq stimulates phospholipase C to increase intracellular free calcium and Gi inhibits adenylate cyclase. Furthermore, the receptor stimulates the mitogen-activated protein kinase pathways. It is ubiquitously and constitutively expressed in healthy tissues. The B2 receptor forms a complex with angiotensin converting enzyme (ACE), and this is thought to play a role in cross-talk between the renin-angiotensin system (RAS) and the kinin-kallikrein system (KKS).
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It is an undecapeptide with the amino acid sequence Arg-Pro-Lys-Pro-Gln-Gln- Phe-Phe-Gly-Leu-Met-NH2. SP binds to all three of the tachykinin receptors, but it binds most strongly to the NK1 receptor. Tachykinin NK1 receptor, often referred to as NK1 receptor, is a member of family 1 (rhodopsin-like) of G protein-coupled receptors and binds to the Gαq protein. NK1 receptor consists of 407 amino acid residues, and it has a molecular weight of 58.000.
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The nerve tissues which communicate with muscles contain a receptor called the nicotinic acetylcholine receptor. Stimulation of these receptors causes a muscular contraction. The anatoxin-a molecule is shaped so it fits this receptor, and in this way it mimics the natural neurotransmitter normally used by the receptor, acetylcholine. Once it has triggered a contraction, anatoxin-a does not allow the neurons to return to their resting state, because it is not degraded by cholinesterase which normally performs this function.
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The 3D structure of the H4 receptor has not been solved yet due to the difficulties of GPCR crystallization. Some attempts have been made to develop structural models of the H4 receptor for different purposes. The first H4 receptor model was built by homology modelling based on the crystal structure of bovine rhodopsin. This model was used for the interpretation of site-directed mutagenesis data, which revealed the crucial importance of Asp94 (3.32) and Glu182 (5.46) residues in ligand binding and receptor activation.
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The protein encoded by the TAS1R1 gene is a G protein-coupled receptor with seven trans-membrane domains and is a component of the heterodimeric amino acid taste receptor T1R1+3. This receptor is formed as a dimer of the TAS1R1 and TAS1R3 proteins. Moreover, the TAS1R1 protein is not functional outside of formation of the 1+3 heterodimer. The TAS1R1+3 receptor has been shown to respond to L-amino acids but not to their D-enantiomers or other compounds.
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The GABA neurotransmitter mediates the fast synaptic inhibition in the central nervous system. When GABA is released from its pre- synaptic cell, it will bind to a receptor (most likely the GABAA receptor) that causes the post-synaptic cell to hyperpolarize (stay below its action potential threshold). This will counteract the effect of any excitatory manipulation from other neurotransmitter/receptor interactions. This GABAA receptor contains many binding sites that allow conformational changes and are the primary target for drug development.
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The neuropeptide S receptor (NPSR) is a member of the G-protein coupled receptor superfamily of integral membrane proteins which binds neuropeptide S (NPS). It was formerly an orphan receptor, GPR154, until the discovery of neuropeptide S as the endogenous ligand. Increased expression of this gene in ciliated cells of the respiratory epithelium and in bronchial smooth muscle cells is associated with asthma. This gene is a member of the G protein- coupled receptor 1 family and encodes a plasma membrane protein.
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The KOR is a type of opioid receptor that binds the opioid peptide dynorphin as the primary endogenous ligand (substrate naturally occurring in the body). In addition to dynorphin, a variety of natural alkaloids, terpenes and other synthetic ligands bind to the receptor. The KOR may provide a natural addiction control mechanism, and therefore, drugs that target this receptor may have therapeutic potential in the treatment of addiction. There is evidence that distribution and/or function of this receptor may differ between sexes.
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ACE inhibitors possess many common characteristics with another class of cardiovascular drugs, angiotensin II receptor antagonists, which are often used when patients are intolerant of the adverse effects produced by ACE inhibitors. ACE inhibitors do not completely prevent the formation of angiotensin II, as blockage is dose-dependent, so angiotensin II receptor antagonists may be useful because they act to prevent the action of angiotensin II at the AT1 receptor, leaving AT2 receptor unblocked; the latter may have consequences needing further study.
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The B2 receptor is a G protein- coupled receptor, probably coupled to Gq and Gi. Gq stimulates phospholipase C to increase intracellular free calcium and Gi inhibits adenylate cyclase. Furthermore, the receptor stimulates the mitogen-activated protein kinase pathways. It is ubiquitously and constitutively expressed in healthy tissues. The B2 receptor forms a complex with angiotensin converting enzyme (ACE), and this is thought to play a role in cross-talk between the renin-angiotensin system (RAS) and the kinin-kallikrein system (KKS).
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The existence of a receptor for transferrin iron uptake had been recognized over half a century back. Earlier two transferrin receptors in humans, transferrin receptor 1 and transferrin receptor 2 had been characterized and until recently cellular iron uptake was believed to occur chiefly via these two well documented transferrin receptors. Both these receptors are transmembrane glycoproteins. TfR1 is a high affinity ubiquitously expressed receptor while expression of TfR2 is restricted to certain cell types and is unaffected by intracellular iron concentrations.
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The muscarinic acetylcholine receptor M1, also known as the cholinergic receptor, muscarinic 1, is a muscarinic receptor that in humans is encoded by the CHRM1 gene. It is localized to 11q13. This receptor is found mediating slow EPSP at the ganglion in the postganglionic nerve, is common in exocrine glands and in the CNS. It is predominantly found bound to G proteins of class Gq that use upregulation of phospholipase C and, therefore, inositol trisphosphate and intracellular calcium as a signalling pathway.
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Macrophage inducible Ca2+-dependent lectin receptor, (abbreviated to Mincle), is a member of the C-type lectin superfamily encoded by the gene CLEC4E. It is a pattern recognition receptor that can recognize glycolipids including mycobacterial cord factor, trehalose-6,6'-dimycolate (TDM). The mincle receptor binds a range of carbohydrate structures, predominantly containing glucose or mannose, and play an important role in recognition of bacterial glycolipids by the immune system. Upon activation by cord factor, Mincle binds the Fc receptor FcRγ and Syk.
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Fig 1. Losartan receptor binding Ang II binds to AT1 receptors via various binding sites. The primary binding site is at the extracellular region of the AT1 receptor where Ang II interacts with residues in the N-terminus of the AT1 receptor and its first and third extracellular loops. The transmembrane helices also contribute to the binding via the C-terminal carboxyl group that interacts with Lys199 in the upper part of helix 5 of the receptor; see figure 1 for details.
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The anti-Müllerian hormone receptor (Müllerian Inhibiting Substance Type II Receptor) can be responsible for persistent Müllerian duct syndrome. Müllerian inhibiting substance type II receptor (MISIIR), also known as the Anti- Müllerian Hormone Receptor, is expressed by ovarian, breast, and prostate cancers and these cancer cells have been reported to apoptose in response to exposure to the Müllerian inhibiting substance (MIS). Antibodies have been developed that specifically target MISIIR and may be useful as vehicles for drugs and toxins for targeted cancer therapy.
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Examples of antagonists, or more appropriately named receptor channel blockers, of the NMDA receptor are APV, amantadine, dextromethorphan (DXM), ketamine, magnesium, tiletamine, phencyclidine (PCP), riluzole, memantine, methoxetamine (MXE), methoxphenidine (MXP) and kynurenic acid. While dizocilpine is generally considered to be the prototypical NMDA receptor blocker and is the most common agent used in research, animal studies have demonstrated some amount of neurotoxicity, which may or may not also occur in humans. These compounds are commonly referred to as NMDA receptor antagonists.
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These neurosteroids have excitatory effects on neurotransmission. They act as potent negative allosteric modulators of the GABAA receptor, weak positive allosteric modulators of the NMDA receptor, and/or agonists of the σ1 receptor, and mostly have antidepressant, anxiogenic, cognitive and memory-enhancing, convulsant, neuroprotective, and neurogenic effects. Major examples include the pregnanes pregnenolone sulfate (PS), epipregnanolone, and isopregnanolone (sepranolone), the androstanes dehydroepiandrosterone (DHEA; prasterone), and dehydroepiandrosterone sulfate (DHEA-S; prasterone sulfate), and the cholestane 24(S)-hydroxycholesterol (NMDA receptor-selective; very potent).
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A number of drugs that work through nuclear receptors display an agonist response in some tissues and an antagonistic response in other tissues. This behavior may have substantial benefits since it may allow retaining the desired beneficial therapeutic effects of a drug while minimizing undesirable side effects. Drugs with this mixed agonist/antagonist profile of action are referred to as selective receptor modulators (SRMs). Examples include Selective Androgen Receptor Modulators (SARMs), Selective Estrogen Receptor Modulators (SERMs) and Selective Progesterone Receptor Modulators (SPRMs).
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Civelli's research is focused on understanding brain function and the identification and study of novel molecules involved in brain activity. He was the first to decipher the structure of a dopamine receptor, the D2 receptor, central to neurobiology. He also uncovered the diversity of dopamine receptor family, identifying the D1 and D5 receptors and discovered the D4 receptor, of importance in psychiatry. Civelli then invented the strategy that uses orphan receptors to discover new neurotransmitters referred to as reverse pharmacology.
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BD1063 or 1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 9 ± 1 nM for the sigma-1 receptor and more than 49 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1063 significantly decreases the convulsivity and lethality of cocaine. In other animal studies, BD1063 blocks the effects of MDMA, and reduces alcohol intake in rodent models of alcoholism.
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Nintedanib is a triple angiokinase inhibitor that targets receptor tyrosine kinases involved in the regulation of angiogenesis: fibroblast growth factor receptor (FGFR), platelet-derived growth factor receptor (PDGFR), and vascular endothelial growth factor receptor (VEGFR), which have also been implicated in the pathogenesis of fibrosis and IPF. In both phase III trials, nintedanib reduced the decline in lung function by approximately 50% over one year. It was approved by the US FDA in October 2014 and authorised in Europe in January 2015.
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One of the first DREADDs was based on the human M3 muscarinic receptor (hM3). Only two point mutations of hM3 were required to achieve a mutant receptor with nanomolar potency for CNO, insensitivity to acetylcholine (ACh) and low constitutive activity and this DREADD receptor was named hM3Dq. M1 and M5 muscarinic receptors have been mutated to create DREADDs hM1Dq and hM5Dq respectively. The most commonly used inhibitory DREADD is hM4Di, derived from the M4 muscarinic receptor that couples with the Gi protein.
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Calreticulin is also found in the nucleus, suggesting that it may have a role in transcription regulation. Calreticulin binds to the synthetic peptide KLGFFKR, which is almost identical to an amino acid sequence in the DNA-binding domain of the superfamily of nuclear receptors. The amino terminus of calreticulin interacts with the DNA-binding domain of the glucocorticoid receptor and prevents the receptor from binding to its specific glucocorticoid response element. Calreticulin can inhibit the binding of androgen receptor to its hormone-responsive DNA element and can inhibit androgen receptor and retinoic acid receptor transcriptional activities in vivo, as well as retinoic acid-induced neuronal differentiation.
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In a culture of hippocampal neurons, CNQX partially inhibited AMPA receptor internalization that was stimulated by AMPA. However, when the hippocampal neurons were treated with CNQX alone, AMPA receptor internalization still took place in both the soma and dendrites. APV (NMDA receptor antagonist) or nimodipine (voltage gated calcium channel blocker) were also not able to block this internalization, suggesting that receptor activation is not a requirement for AMPA receptor endocytosis. The type of AMPA receptors endocytosed as a result of CNQX stimulation can also be identified using CNQX. In HEK cells tagged with GluR subunits, CNQX stimulates the internalization of GluR1 and GluR2 receptors.
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Interleukin-17 receptor (IL-17R) is a cytokine receptor which belongs to new subfamily of receptors binding proinflammatory cytokine interleukin 17A, a member of IL-17 family ligands produced by T helper 17 cells (Th17). IL-17R family consists of 5 members: IL-17RA, IL-17RB, IL-17RC, IL-17RD and IL-17RE. Functional IL-17R is a transmembrane receptor complex usually consisting of one IL-17RA, which is a founding member of the family, and second other family subunit, thus forming heteromeric receptor binding different ligands. IL-17A, a founding member of IL-17 ligand family binds to heteromeric IL-17RA/RC receptor complex.
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This receptor is a heterodimer receptor complex consisting of alpha IL-4 receptor (IL-4Rα) and alpha Interleukin-13 receptor (IL-13R1). The high affinity of IL-13 to the IL-13R1 leads to their bond formation which further increase the probability of a heterodimer formation to IL-4R1 and the production of the type 2 IL-4 receptor. Heterodimerization activates both the STAT6 and the IRS. STAT6 signaling is important in initiation of the allergic response. Most of the biological effects of IL-13, like those of IL-4, are linked to a single transcription factor, signal transducer and activator of transcription 6 (STAT6).
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Activated glucocorticoid receptor has effects that have been experimentally shown to be independent of any effects on transcription and can only be due to direct binding of activated glucocorticoid receptor with other proteins or with mRNA. For example, Src kinase which binds to inactive glucocorticoid receptor, is released when a glucocorticoid binds to glucocorticoid receptor, and phosphorylates a protein that in turn displaces an adaptor protein from a receptor important in inflammation, epidermal growth factor, reducing its activity, which in turn results in reduced creation of arachidonic acid - a key proinflammatory molecule. This is one mechanism by which glucocorticoids have an anti- inflammatory effect.
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The liver X receptor (LXR) is a member of the nuclear receptor family of transcription factors and is closely related to nuclear receptors such as the PPARs, FXR and RXR. Liver X receptors (LXRs) are important regulators of cholesterol, fatty acid, and glucose homeostasis. LXRs were earlier classified as orphan nuclear receptors, however, upon discovery of endogenous oxysterols as ligands, they were subsequently deorphanized. Two isoforms of LXR have been identified and are referred to as LXRα and LXRβ. The liver X receptors are classified into subfamily 1 (thyroid hormone receptor-like) of the nuclear receptor superfamily, and are given the nuclear receptor nomenclature symbols NR1H3 (LXRα) and NR1H2 (LXRβ) respectively.
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Studies of the direct effects of EP3 receptor activation on cancer in animal and tissue models give contradictory results suggesting that this receptor does not play an important role in Carcinogenesis. However, some studies suggest an indirect pro-carcinogenic function for the EP3 receptor: The growth and metastasis of implanted Lewis lung carcinoma cells, a mouse lung cancer cell line, is suppressed in EP33 receptor deficient mice. This effect was associated with a reduction in the levels of Vascular endothelial growth factor and matrix metalloproteinase-9 expression in the tumor's stroma; expression of the pro-lymphangiogenic growth factor,VEGF-C and its receptor, VEGFR3; and a tumor-associated angiogenesis and lymphangiogenesis.
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When ligands bind to the receptor, the ion channel portion of the receptor opens, allowing ions to pass across the cell membrane. Acetylcholine is a neurotransmitter synthesized from dietary choline and acetyl-CoA (ACoA), and is involved in the stimulation of muscle tissue in vertebrates as well as in some invertebrate animals. In vertebrate animals, the acetylcholine receptor subtype that is found at the neuromuscular junction of skeletal muscles is the nicotinic acetylcholine receptor (nAChR), which is a ligand-gated ion channel. Each subunit of this receptor has a characteristic "cys-loop", which is composed of a cysteine residue followed by 13 amino acid residues and another cysteine residue.
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The IL-15 receptor is composed of three subunits: IL-15R alpha, CD122, and CD132. Two of these subunits, CD122 and CD132, are shared with the receptor for IL-2, but IL-2 receptor has an additional subunit (CD25). The shared subunits contain the cytoplasmic motifs required for signal transduction, and this forms the basis of many overlapping biological activities of IL15 and IL2, although in vivo the two cytokines have separate biological effects. This may be due to effects of the respective alpha chains, which are unique to each receptor, the kinetics and affinity of cytokine-cytokine receptor binding, or due to the availability and concentration of each cytokine.
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Type I IFN receptor forms a ternary complex, composed of its two subunits IFNAR1 and IFNAR2, and a type I IFN ligand. Ligand binding to either subunit is required for and precedes dimerization and activation of the receptor. Each subunit of IFNAR contains an N-terminal ligand binding domain (with two or four fibronectin type II-like subdomains, for IFNAR2 and IFNAR1, respectively), a transmembrane (TM) domain, and a cytoplasmic domain. Each type I IFN ligand contains a "hotspot", or a sequence of conserved amino acids that are involved in binding to the receptor, specifically the high affinity receptor IFNAR2, which determines the affinity of each ligand for the receptor.
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PDGF-AA binds only to PDGFR-αα, while PDGF-BB is the only PDGF that can bind all three receptor combinations with high affinity. Dimerization is a prerequisite for the activation of the kinase. Kinase activation is visualized as tyrosine phosphorylation of the receptor molecules, which occurs between the dimerized receptor molecules (transphosphorylation). In conjunction with dimerization and kinase activation, the receptor molecules undergo conformational changes, which allow a basal kinase activity to phosphorylate a critical tyrosine residue, thereby "unlocking" the kinase, leading to full enzymatic activity directed toward other tyrosine residues in the receptor molecules as well as other substrates for the kinase.
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The full length endoglin will bind to the TGF beta receptor complex whether TGF beta is bound or not, but the truncated forms of endoglin have more specific binding. The amino acid (aa) region 437–558 in the extracellular domain of endoglin will bind to TGF beta receptor II. TGF beta receptor I binds to the 437-588 aa region and to the aa region between 437 and the N-terminus. Unlike TGF beta receptor I which can only bind the cytoplasmic tail when its kinase domain is inactive, TGF beta receptor II can bind endoglin with an inactive and active kinase domain. The kinase is active when it is phosphorylated.
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The σ1 receptor is defined by its unique pharmacological profile. In 1976 Martin reported that the effects of N-allylnormetazocine (SKF-10,047) could not be due to activity at the μ and κ receptors (named from the first letter of their selective ligands morphine and ketazocine, respectively) and a new type of opioid receptor was proposed; σ (from the first letter of SKF-10,047). The opioid classification was eventually dropped however resulting from it not possessing the canonical opioid G-protein coupled receptor structure and the receptor was later referred to as simply the σ1 receptor. It was found to have affinity for the (+)-stereoisomers of several benzomorphans (e.g.
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The Carlson lab studies insect chemosensation using the model organism Drosophila. Significant contributions to the field include discovery of the olfactory receptor genes in insects using the Drosophila genome, called the Odorant Receptor (Or) gene family, followed by the discovery of the insect taste receptor genes, called the Gustatory Receptor (Gr) gene family, a system to deorphanize insect odorant receptors referred to as the "empty neuron" system, using which a study identified ligands for most of the Drosophila Olfactory Receptor (Or) repertoire and a similar study that characterized the Or repertoire of the Anopheles gambiae mosquito. Carlson lab research has also been featured in Scientific American.
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Both are addictive drugs, cocaine being a stimulant and phencyclidine a hallucinogen. In studying their effects on acetylcholine receptors, Hess found that both drugs inhibited the receptor and affected its equilibrium, though via different mechanisms. His findings were published in his 1982 paper “Cocaine and Phencyclidine Inhibition of the Acetylcholine Receptor: Analysis of the Mechanisms of Action Based on Measurements of Ion Flux in the Millisecond-to-Minutes Time Region.” He continued to explore different techniques for studying the acetylcholine receptor such as the one described in his paper “Acetylcholine Receptor (from Electrophorus electricus): A Comparison of Single-Channel Current Recordings and Chemical Kinetic Measurements.” He used a single-channel measurement technique to determine the currents through the channels of the acetylcholine receptor and the lifetimes of the receptor states.
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In response to Turin's 2013 paper, involving deuterated and undeuterated isotopomers of the musk cyclopentadecanone, Block et al. in a 2015 paper in PNAS report that the human musk-recognizing receptor, OR5AN1, identified using a heterologous olfactory receptor expression system and robustly responding to cyclopentadecanone and muscone (which has 30 hydrogens), fails to distinguish isotopomers of these compounds in vitro. Furthermore, the mouse (methylthio)methanethiol-recognizing receptor, MOR244-3, as well as other selected human and mouse olfactory receptors, responded similarly to normal, deuterated, and carbon-13 isotopomers of their respective ligands, paralleling results found with the musk receptor OR5AN1. Based on these findings, the authors conclude that the proposed vibration theory of olfaction does not apply to the human musk receptor OR5AN1, mouse thiol receptor MOR244-3, or other olfactory receptors examined.
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The deduced amino acid sequences revealed that ALK was a novel receptor tyrosine kinase (RTK), having an extracellular ligand-binding domain, a transmembrane domain, and an intracellular tyrosine kinase domain. While the tyrosine kinase domain of human ALK shares a high degree of similarity with that of the insulin receptor, its extracellular domain is unique among the RTK family in containing two MAM domains (meprin, A5 protein and receptor protein tyrosine phosphatase mu), an LDLa domain (low-density lipoprotein receptor class A) and a glycine-rich region. Based on overall homology, ALK is closely related to the leukocyte receptor tyrosine kinase (LTK) and, together with the insulin receptor, forms a subgroup in the RTK superfamily. The human ALK gene encodes a protein 1,620 amino acids long with a molecular weight of 180 kDa.
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Leukotriene B4 receptor 2, also known as BLT2, BLT2 receptor, and BLTR2, is an Integral membrane protein that is encoded by the LTB4R2 gene in humans and the Ltbr2 gene in mice. Discovered several years after the leukotriene B4 receptor 1 (BLT1), BLT2 receptor binds leukotriene B4 (LTB4) with far lower affinity than the BLT1 receptor does and therefore has been termed the low affinity LTB4 receptor. Sometime after its initial discovery, the BLT2 receptor was shown to bind and become activated by several other arachidonic acid metabolites, one of which, 12-hydroxyheptadecatrienoic acid (12-HHT), has 10- to 100-fold higher affinity for it than does LTB4; 12-HHT fails to bind or activate BLT1 receptors. While BLT2 receptors have some actions similar to BLT1 receptors, they have other actions which clearly oppose those of BLT1 in regulating inflammation and allergic responses; BLT2 receptors also have actions that extend beyond those of BLT1 receptors.
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Molecular neuropharmacology involves the study of neurons and their neurochemical interactions, and receptors on neurons, with the goal of developing new drugs that will treat neurological disorders such as pain, neurodegenerative diseases, and psychological disorders (also known in this case as neuropsychopharmacology). There are a few technical words that must be defined when relating neurotransmission to receptor action: # Agonist – a molecule that binds to a receptor protein and activates that receptor # Competitive antagonist – a molecule that binds to the same site on the receptor protein as the agonist, preventing activation of the receptor # Non- competitive antagonist – a molecule that binds to a receptor protein on a different site than that of the agonist, but causes a conformational change in the protein that does not allow activation. The following neurotransmitter/receptor interactions can be affected by synthetic compounds that act as one of the three above. Sodium/potassium ion channels can also be manipulated throughout a neuron to induce inhibitory effects of action potentials.
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Scavenger receptor class B type 1 (SRB1) also known as SR-BI is a protein that in humans is encoded by the SCARB1 gene. SR-BI functions as a receptor for high-density lipoprotein.
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Specifically, GABAB receptors modulate excitatory and inhibitory inputs to the LSO. Whether the GABAB receptor functions as excitatory or inhibitory for the postsynaptic neuron, depends on the exact location and action of the receptor.
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The growth-hormone-releasing hormone receptor (GHRHR) is a G-protein-coupled receptor that binds growth hormone-releasing hormone. The GHRHR activates a Gs protein that causes a cascade of cAMP via adenylate cyclase.
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This model was arguably flawed in that it did not incorporate the equilibrium between the inactivated agonist-bound-receptor and the activated agonist-bound-receptor that is shown in the del Castillo Katz model.
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Adiponectin receptor 2 (AdipoR2) is a protein which in humans is encoded by the ADIPOR2 gene. It is a member of the progestin and adipoQ receptor (PAQR) family, and is also known as PAQR2.
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Spiroxatrine is a drug which acts as a selective antagonist at both the 5-HT1A receptor and the α2C adrenergic receptor. It is an analog of spiperone and also has some dopamine antagonist effects.
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Pazopanib is a multiple kinase inhibitor that limits tumor growth by targeting angiogenesis via inhibition of enzymes including vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), c-KIT and FGFR.
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Via the androgen receptor, androgens play a key role in the maintenance of male skeletal integrity. The regulation of this integrity by androgen receptor (AR) signaling can be attributed to both osteoblasts and osteocytes.
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D1-D2 dopamine receptor heteromer formation is observed. D1 dopamine receptor signaling is necessary to initiate the gene expression changes in the nucleus accumbens that are critical for the development and maintenance of addiction.
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Adiponectin receptor 1 (AdipoR1) is a protein which in humans is encoded by the ADIPOR1 gene. It is a member of the progestin and adipoQ receptor (PAQR) family, and is also known as PAQR1.
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They are more likely to be diagnosed with hormone-receptor positive tumors, with about six out of seven cases being estrogen-receptor positive. The overall prognosis is worse for male than for female patients.
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Smads are a class of intracellular signalling proteins and transcription factors for the TGF-β family of signalling molecules. This pathway conceptually resembles the Jak- STAT signal transduction pathway characterized in the activation of cytokine receptors implicated, for example, in the B cell isotype switching pathway. As previously stated, the binding of the TGF-β ligand to the TGF-β receptor, the type 2 receptor kinase phosphorylates and activates the type 1 receptor kinase that activates a signaling cascade. In the case of Smad, receptor-activated Smads are phosphorylated by the type 1 TGF-β receptor kinase, and these go on to complex with other Smads, which is able to translocate into the cell nucleus to induce transcription of different effectors. More specifically, activated TGF-β complexes bind to the type 2 domain of the TGF-β receptor which then recruits and phosphorylates a type 1 receptor. The type 1 receptor then recruits and phosphorylates a receptor regulated SMAD (R-SMAD). The R-SMAD then binds to the common SMAD (coSMAD) SMAD4 and forms a heterodimeric complex. This complex then enters the cell nucleus where it acts as a transcription factor for various genes, including those to activate the mitogen-activated protein kinase 8 pathway, which triggers apoptosis.
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The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication. Macimorelin is a growth hormone secretagogue receptor (ghrelin receptor) agonist causing release of growth hormone from the pituitary gland.
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Because of this, it is believed the protruding protein may act as a receptor. This receptor activity has been known to occur in many plant viruses, but has not yet been seen in this order.
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TSLP signals through a heterodimeric receptor complex composed of the thymic stromal lymphopoietin receptor CRLF2 and the IL-7R alpha chain. After binding STAT5 phosphorylation is induced, resulting in the expression of upstream transcription factors.
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The olfactory receptor gene family is the largest in the genome. The nomenclature assigned to the olfactory receptor genes and proteins for this organism is independent of other organisms. OR2M3 has a copper binding pocket.
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In a feedback mechanism, these activated kinases phosphorylate the receptor. The longer the receptor remains active the more kinases are activated and the more receptors are phosphorylated. Other pathways of signaling exist for the LHCGR.
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While it acts at alpha- adrenergic, dopaminergic, and serotonin receptors (the 5-HT2 receptor), it exerts on the uterus (and other smooth muscles) a powerful stimulant effect not clearly associated with a specific receptor type.
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Recent studies have revealed a truncated isoform of the TrkB receptor (t-TrkB) may act as a dominant negative to the p75 neurotrophin receptor, inhibiting the activity of p75, and preventing BDNF-mediated cell death.
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"Receptor Ectodomain Shedding" - Tumor- necrosis factor alpha converting enzyme (T.A.C.E.) proteolytically cleaves the extracellular domain off of (two) growth hormone receptor(s) to release the soluble carrier-protein growth hormone-binding protein. Adapted from Fisker.
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TAS2R50 belongs to the large TAS2R receptor family. TAS2Rs are expressed on the surface of taste receptor cells and mediate the perception of bitterness through a G protein-coupled second messenger pathway. See also TAS2R10.
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This gene (IFNGR2) encodes the non-ligand-binding beta chain of the gamma interferon receptor. Human interferon-gamma receptor is a multimer of two IFN-γR1 chains (encoded by IFNGR1) and two IFN-γR2 chains.
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Progress in purification of the cholinergic receptor protein from Electrophorus electricus by affinity chromatography. FEBS Lett. 28., 96-100. allowed the proposition that the receptor was a pentameric protein,Hucho F., Changeux J.-P. (1973).
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Quipazine is a piperazine drug used in scientific research. It is a moderately selective serotonin receptor receptor agonist, binding to a range of different serotonin receptors, but particularly to the 5-HT2A and 5-HT3.
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Alvameline (Lu 25-109) is a M1 receptor agonist and M2/M3 receptor antagonist that was under investigation for the treatment of Alzheimer's disease, but produced poor results in clinical trials and was subsequently discontinued.
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Hall, F.S., Sora, I., & Uhl, G.R. (2001). Ethanol consumption and reward are decreased in mu-opiate receptor knockout mice. Psychopharmacology, 154, 43–49. Knockouts of CB1 cannabinoid receptor demonstrated a lack of conditioned place preference.
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Retinoic acid receptor beta has been shown to interact with NR4A2.
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Retinoic acid receptor gamma has been shown to interact with NCOR1.
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EFCAB6 has been shown to interact with PARK7 and Androgen receptor.
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C1QTNF1 has been shown to interact with Arginine vasopressin receptor 2.
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Compared with unbiased agonists RB-64 evokes considerably less receptor internalisation.
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Melanocortin 2 Receptor accessory protein (MRAP) traps MC5R protein inside cells.
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The primary endogenous agonist of the human CB1 receptor is anandamide.
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TRIP4 has been shown to interact with Nuclear receptor coactivator 1.
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SHC2 has been shown to interact with Kinase insert domain receptor.
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TMF1 has been shown to interact with FER and Androgen receptor.
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RNF8 has been shown to interact with Retinoid X receptor alpha.
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It has little to no effect on the κ-opioid receptor.
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Retinoid X receptor gamma has been shown to interact with ITGB3BP.
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Luteinizing hormone/choriogonadotropin receptor has been shown to interact with GIPC1.
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Additionally, a melanopsin based receptor has been linked to migraine pain.
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TENC1 has been shown to interact with AXL receptor tyrosine kinase.
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GPRASP1 (gene) has been shown to interact with Delta Opioid receptor.
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Azemiopsin is a blocker of the nicotinic acetylcholine receptor in muscle.
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Metabotropic glutamate receptor 7 has been shown to interact with PICK1.
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Beta-3 adrenergic receptor has been shown to interact with Src.
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All these proteins function as stress-induced ligands for NKG2D receptor.
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Interleukin 8 receptor, alpha has been shown to interact with GNAI2.
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The 5-HT2C receptor has been shown to interact with MPDZ.
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Arginine vasopressin receptor 2 has been shown to interact with C1QTNF1.
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Phaclofen, or phosphonobaclofen, is a selective antagonist for the GABAB receptor.
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AXL receptor tyrosine kinase has been shown to interact with TENC1.
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FNTA has been shown to interact with TGF beta receptor 1.
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AKAP12 has been shown to interact with Beta-2 adrenergic receptor.
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SART3 has been shown to interact with RNPS1 and Androgen receptor.
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For instance, methamphetamine acts as an agonist of sigma-1 receptor.
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Draquinol is a beta blocker with selectivity for the β1 receptor.
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