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August 2022 GPR3 expression in retinal ganglion cells contributes to neuron survival and accelerates GPR3 is unique in its ability to constitutively activate the Gαs protein without a ligand, which elevates Our earlier reports suggested that GPR3 enhances both neurite outgrowth and neuronal survival. GPR3 was relatively highly expressed in retinal ganglion cells (RGCs). Evaluation of the effect of GPR3 on axonal regeneration using GPR3 knockout mice revealed that GPR3 in

Our previous work demonstrated that GPR3-mediated β-arrestin signaling modulates amyloid-β (Aβ) generation in vitro and that Gpr3 deficiency ameliorates Aβ pathology in vivo. However, Gpr3-deficient mice display several adverse phenotypes, including elevated anxiety-like behavior consequences of selective elimination of GPR3-mediated β-arrestin signaling in vivo. In contrast to Gpr3-deficient mice, G protein-biased GPR3 mice do not display elevated anxiety levels

roles of focal adhesion kinase (protein tyrosine kinase 2, PTK2), the shear-dependent collagen receptor GPR56 peptides that interfered with integrin αIIb binding (pCIB and pCIBm) or mimicked the activation of GPR56 integrin αIIbβ3, and CIB1 in collagen- and GPVI-dependent thrombus formation, which is modulated by GPR56

Here, we report that the Ovarian Cancer G-Protein Coupled Receptor1 (OGR1 or GPR68) has dual roles in

into phase 3 Certa Therapeutics Announces International Non-Proprietary Name for its First-in-class GPR68 (OX2R) Agonist, ORX750, in Acutely Sleep-Deprived Healthy Volunteers Cumulus raising $50M, spinning GPR68 position Adhesion GPCRs Loss of cardiomyocyte-specific Adhesion G Protein Coupled Receptor G1 (ADGRG1/GPR56

adhesion-GPCR ADGRF5 fuels breast cancer progression by suppressing the MMP8-mediated antitumorigenic effects GPR56 vitro and in vivo GPCRs in Neuroscience Elucidating the activation mechanism of the proton-sensing GPR68

mechanisms governing G protein coupling selectivity of GPCRs Location-biased activation of the proton-sensor GPR65 uncoupled from receptor trafficking GPCR Binders, Drugs, and more An inverse agonist of orphan receptor GPR61

Adhesion GPCRs Downstream signaling of the disease associated mutations on GPR56/ADGRG1. Summit, Boston MA Pathios Therapeutics Unveils PTT-4256, a Highly Potent and Selective Inhibitor of GPR65

Activation of the proton-sensing GPCR, GPR65 on fibroblast-like synoviocytes contributes to inflammatory Biochemist/Structural Biologist GPCR Activation and Signaling Activation of the proton-sensing GPCR, GPR65

approach has been conducted to reveal the functional importance of each residue in proton recognition in GPR68 The result suggested that, in contrast to other proton-sensitive channels and receptors, GPR68 did not

studying these proteins and this year the transmembrane structures of the aGPCRs ADGRL3/Lphn3, ADGRG1/GPR56 , ADGRG5/GPR114, ADGRD1/GPR133, ADGRF1/GPR110, ADGRG2/GPR64, and ADGRG4/GPR112 were reported in their

medaka Oryzias melastigma Industry News Cumulus Oncology and leadXpro Achieve Critical Milestone in GPR68

Schihada and his lab team developed fluorescent analogues for real-time binding studies of orphan GPCR GPR3 Development of Fluorescent AF64394 Analogues Enables Real-Time Binding Studies for the Orphan Class A GPCR GPR3

Belousoff et al. for their work on Lipid-Dependent Activation of the Orphan G Protein-Coupled Receptor GPR3 histamine H3 receptor isoforms Lipid-Dependent Activation of the Orphan G Protein-Coupled Receptor, GPR3

GPCRs in Neuroscience Whole genome sequencing across clinical trials identifies rare coding variants in GPR68

, and Taste GPRASP1 loss-of-function links to arteriovenous malformations by endothelial activating GPR4

Structural Biology and Drug Discovery Approaches Altered PLCβ/IP3/Ca2+ Signaling Pathway Activated by GPRCs

G-protein-coupled receptor rhodopsin activation GPCR Binders, Drugs, and more Chimeric antigens displaying GPR65

GPCR Classes Pathios Therapeutics Announces Dosing of First Patient in Phase 1/2 Clinical Study of GPR65

roles of DRY and NPxxY motifs in selective activation of downstream signalling by the apelin receptor GPR68

and Signaling GPRASP1 loss-of-function links to arteriovenous malformations by endothelial activating GPR4

N-terminus in discriminating the endocytic effects of opioid agonist drugs GPCRs in Oncology and Immunology GPR56

glycosaminoglycan binding, CXCR3A signaling and lymphocyte chemotaxis, while retaining angiostatic activity GPR68

pharmacogenomics Antibodies expand the scope of angiotensin receptor pharmacology Chimeric antigens displaying GPR65

Hexahydroquinoline Derivatives are Selective Agonists for the Adhesion G Protein-Coupled Receptor ADGRG1/GPR56

GPCR Binders, Drugs, and more An antibody-drug conjugate targeting GPR56 demonstrates efficacy in preclinical

Neuroscience Molecular insights into orphan G protein-coupled receptors relevant to schizophrenia Re-routing GPR56

contributes to immune characteristics of microenvironment and process of EBV-induced lymphomagenesis GPR56