Some of these are GPR6, GPR37 and GPR139 , which participate in motor control, neuroprotection and metabolic GPR6 has been linked to neuroprotective functions and is now being investigated for its role in Parkinson

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

Explore discussion ➤ This Week’s Scientific Highlight GPR61, implicated in appetite and body weight regulation Premium This is what Premium Members are reading this week: 20 classified papers including one on 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

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

it spans an unusually wide slice of the field: Antifibrotic and anti-inflammatory targets, including GPR68

week: Decoding ADGRE5 signaling; Eli Lilly’s obesity pill vs Novo’s Wegovy; Certa Therapeutics patents GPR68

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

Must-read publications:  OX2R dynamics; GPR68 nociception.

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

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

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

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

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

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

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

Must-read publications:  β-arrestin2-biased allosteric modulator for pain beyond opioids & GPR3 regulated