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October 2022 GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral GPR125 (ADGRA3), an orphan adhesion GPCR, has been shown to modulate planar cell polarity in gastrulating Here, we show that human GPR125 likely undergoes cis-autoproteolysis when expressed in canine kidney Furthermore, in polarized MDCK cells, GPR125 is exclusively recruited to the basolateral domain of the The recruitment likely requires the C-terminal PDZ-domain-binding motif of GPR125 and its interaction

presented this important pre-clinical work at SIRS2022 confirming the ability of the highly selective novel GPR52 important interplay between the adenosinergic and dopaminergic systems and suggests the potential for GPR52

October 2022 GPR15 expressed in T lymphocytes from RA patients is involved in leukocyte chemotaxis to GPR15 is a G protein-coupled receptor (GPCR) located on chromosome 3 and has similarity in its sequence The expression of GPR15 and c10orf99/gpr15l mRNA was analyzed by RT-qPCR. +GPR15+ T cell frequency comparing RA patients versus control subjects by flow cytometry. A higher expression in the mRNA for GPR15 was identified in early RA subjects.

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous GPR15 signals through the Gi/o pathway to decrease intracellular cyclic adenosine 3',5'-monophosphate However, the activation profiles of the GPR15 receptor within Gi/o subtypes have not been examined. Here, GPR15L(25-81) and GPR15L(71-81) are used as pharmacological tool compounds to delineate the GPR15 The results show that the GPR15 receptor preferentially couples to Gi/o rather than other pathways in

Adhesion GPCRs A screen of pharmacologically active compounds to identify modulators of the Adgrg6/Gpr126 Inverse agonism of lysophospholipids with cationic head groups at Gi-coupled receptor GPR82. Sosei Heptares Doses First Subject in Phase I Trial with HTL0048149, a First-in-Class GPR52 Agonist for

August 2022 "GPR21 is an orphan and constitutively active receptor belonging to the superfamily of G-Protein GPR21 couples to the Gq family of G proteins and is expressed in macrophages. Studies of GPR21 knock-out mice indicated that GPR21 may be involved in promoting macrophage migration The aim of this study was to evaluate the role of GPR21 in human macrophages, analyzing (i) its involvement GPR21 expression was evaluated at gene and protein level, the signalling pathway was investigated by

addition, hearing loss can be caused by mutations of certain GPCRs, such as Vlgr1, Gpr156, S1P2, and Gpr126

, Demet Araç, et al. for their work on The far extracellular CUB domain of the adhesion GPCR ADGRG6/GPR126 peristalsis and labels tick midgut muscles The far extracellular CUB domain of the adhesion GPCR ADGRG6/GPR126

Adhesion GPCRs Collagen VI Is a Gi-Biased Ligand of the Adhesion GPCR GPR126/ADGRG6.

Adhesion GPCRs Adhesion G Protein-Coupled Receptor Gpr126 (Adgrg6) Expression Profiling in Diseased Mouse

G-protein-coupled receptor mayo/CG11318 controls midgut development in Drosophila Structure, ligands, and roles of GPR126

Cryo-EM structures of orphan GPR21 signaling complexes.

sucralose increases β-arrestin signaling at the constitutively active orphan G protein-coupled receptor GPR52

GPCRs in Cardiology, Endocrinology, and Taste G-protein coupled receptor 19 (GPR19) knockout mice display

kidney injury GPCR Binders, Drugs, and more High-throughput virtual screening of potential inhibitors of GPR52

Taste The full-length TSH receptor is stabilized by TSH ligand Cardiomyocyte-specific overexpression of GPR22

RAMP and MRAP accessory proteins have selective effects on expression and signalling of the CB1, CB2, GPR18

Cryo-EM structure of G-protein-coupled receptor GPR17 in complex with inhibitory G protein.

Orexin Receptor mRNA Expression Visualized by Branched In Situ Hybridization Chain Reaction Orphan GPR52

sucralose increases β-arrestin signaling at the constitutively active orphan G protein-coupled receptor GPR52

Cryo-EM structure of orphan G protein-coupled receptor GPR21.

aGPCRs ADGRL3/Lphn3, ADGRG1/GPR56, ADGRG5/GPR114, ADGRD1/GPR133, ADGRF1/GPR110, ADGRG2/GPR64, and ADGRG4/GPR112