Orphan GPCR
Rrphan G protein-coupled receptor
Orphan GPCRs (orphan G protein-coupled receptors) are receptors lacking endogenous ligands. GPCRs are th largest family of transmembrane receptors and have over the past decades developed into highly successful drug targets. However, many GPCRs are still orphans and the function is enigmatic. Orphan GPCRs account for ∼30% of the ∼400 non-olfactory human GPCRs. In terms of orphan GPCR ligands, initial efforts focused on identifying novel neuropeptides since orphan GPCR expression was located primarily in the brain. G protein coupling of unliganded orphan GPCRs—GPR22, GPR137b, GPR88, GPR156, GPR158, GPR179, GPRC5D and GPRC6A—with pathophysiological association were accurately detected using luciferase reporter assays[1][2].
References:
- [1]. Wang T, et, al. Orphan GPCR GPRC5C Facilitates Angiotensin II-Induced Smooth Muscle Contraction . Circ Res. 2024 May 10;134(10):1259-1275. [Content Brief]
- [2]. Jobe A, et, al. Orphan G protein-coupled receptors: the ongoing search for a home. Front Pharmacol. 2024 Feb 29:15:1349097. [Content Brief]
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Orphan GPCR Related Products (25)
Related Products (25)
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Anti-EMR2 Antibody
0 ImagesCat. No.: HY-P992226
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GPR34 agonist 1
0 ImagesCat. No.: HY-164641CAS No.: 2459994-71-7GPR34 agonist 1 is a G-protein coupled receptor 34 agonist that enhances fibrillar Aβ uptake in mouse primary microglia with an EC50 of 5 nM.GPR34 agonist 1 selectively activates Gi/o-coupled GPR34, reduces intracellular cyclic adenosine monophosphate levels, and requires functional TREM2 signaling.GPR34 agonist 1 induces microglial Aβ fibril phagocytosis and chemotaxis, enhances microglial uptake and clearance of amyloid β fibrils, and increases microglial Aβ fibril uptake in vivo and in human induced pluripotent stem cell-derived microglia.GPR34 agonist 1 can be used for the research of Alzheimer disease.
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GPR61 Inverse agonist 2
0 ImagesCat. No.: HY-182270GPR61 Inverse agonist 2 is a selective GPR61 inverse agonist with human IC50 of 6.2 nM and mouse IC50 of 20 nM, human Ki of 0.21 nM, and mouse Ki of 0.72 nM. GPR61 Inverse agonist 2 binds to an induced intracellular allosteric pocket of GPR61, disrupts receptor-Gαs interactions, and abolishes GPR61 constitutive activity. GPR61 Inverse agonist 2 does not alter food intake or body weight in healthy mice. GPR61 Inverse agonist 2 can be used for the research of cachexia/sarcopenia.
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Anti-CD97 Antibody
0 ImagesCat. No.: HY-P991934Anti-CD97 Antibody is an antibody against human CD97.
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PSB-CB-27
0 ImagesCat. No.: HY-159161CAS No.: 2237222-16-9PSB-CB-27 is a potent and selective GPR18 inhibitor with an IC50 of 0.65 μM. PSB-CB-27 shows selectivity over Human GPR55, Human CB1 receptor, and Human CB2 receptor. PSB-CB-27 leads to a complete blockade of Δ9-Tetrahydrocannabinol (THC)-induced GPR18 activation. PSB-CB-27 can be used for inflammatory diseases and cancer immunotherapy research.
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