Prior to this report we did not know how different serotonin receptor subtypes which share high sequence , suggesting that the selectivity of the G-protein lies in intrinsic features of the receptor rather /6/7-Gs coupled receptors have a cytosolic TM5 that is on average 5.7 residues longer and a TM6 that is 7.5 residues shorter compared to 5-HT1/4 receptors that couple to Gi/o. o yielded similar results, TM5 was 5.6 ± 1.5 residues longer while TM6 was 2.6 ± 1.6 residues shorter

November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially contributes to the biased signaling generated by three endogenous ligands of the GPCR CXC chemokine receptor In CD8 + T cells, the chemokines promote unique transcriptional responses predicted to regulate inflammatory observed at CXCR3, which has important implications for drugs targeting chemokine receptors and other Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

September 2022 "Over 100 mutations in the rhodopsin gene have been linked to a spectrum of retinopathies that include retinitis pigmentosa and congenital stationary night blindness. to retinal. (ΔN73, S131P, and R135G) and show that two of these retain residual function in vitro. of retinopathy variants and their response to retinal."

They are G-protein-coupled receptors and bind as ligand retinal, which is bound covalently to a lysine The pipeline compiles and aligns sequences from public sources, reconstructs the phylogeny, prunes rogue sequences, and visualizes the resulting tree. The gluopsins are mainly dragonfly and butterfly opsins, closely related to the RGR-opsins and the retinochromes However, what their particular function is, remains to be seen."

November 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed this work, molecular docking screens for allosteric modulators targeting the metabotropic glutamate receptor The mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system from 0.43 to 8.6 μM, corresponding to a hit rate of 9%. Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures We then mapped the 394 GPCR X-ray structures available at the time of the analysis (September 2020). Results show that for each of the 21 structures with bound ligands there exist many other GPCRs that Results confirm the possibility of specifically targeting these sites across GPCRs for allosteric modulation Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer However, current investigations have now recognized that in addition to GPCR arresting (hence the name arrestin). β-Arrestins are adaptor proteins that control the recruitment, activation, and scaffolding This review delivers a concise overview of the role of β-arrestins with a primary emphasis on the signaling Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

G protein-coupled receptors (GPCRs) are crucial receptors that regulate a wide range of physiological Recently, several GPCRs have been found to play important roles in the cochlea. Frizzleds and Lgrs are dominant GPCRs that regulate stem cell self-renew abilities. Here, we review the key findings of GPCR in the cochlea and discuss the role of GPCR in the cochlea, Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter

October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance in a wide range of physiological functions and in a large number of Food and Drug Administration (FDA and mechanism of action, there is a greater understanding of how effector molecules interact with a receptor This review aims to explore the signaling pathways, dynamic structures, and physiological relevance in Read more at the source #DrGPCR #GPCR #IndustryNews

Past work has produced conflicting results with respect to the effects of pro-inflammatory conditions Thus, we systematically investigated the relationship between the concentration of two distinct pro-inflammatory Furthermore, we demonstrate that the efficacy of different synthetic cannabinoid treatments with respect different pro-inflammatory stimuli influence the capacity of microglia to synthesize, degrade, and respond Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent in primary hepatocytes "A number of G protein-coupled receptors (GPCRs) are now thought to use endocytosis We tested if this is true for the glucagon receptor (GCGR), which mediates physiological regulation of Together, these results implicate the endosomal signaling paradigm in metabolic regulation by glucagon Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Neisseria meningitidis is a Gram-negative opportunistic pathogen that is responsible for N-acyltransferase encoded in the obligate human pathogen N. meningitidis and identified 30 N-acyl amides with representative members serving as agonists of the G-protein coupled receptor (GPCR) S1PR4. Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Heterotrimeric G proteins couple activated G protein-coupled receptors (GPCR) to intracellular function independently of GPCR activation upon acquiring mutations that prevent GTPase activity and result Treatment of cells with YM failed to inhibit signaling by these PM-restricted αqQ209L. αqQ209L, resulting in increased binding to βγ and decreased binding to regulator RGS2, and effectors Read more at the source #DrGPCR #GPCR #IndustryNews

Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets The adenosine A1 and A2A receptors are expressed in the human brain and have a proposed involvement in Targeting these receptors preclinically can mitigate pathogenic β-amyloid and tau neurotoxicity whilst potential of A1 and A2A receptors. Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental hypertension and proteinuria, with a worldwide incidence of 3–8% and high maternal mortality, is a risk Given the great value of the secretin/adhesion (Class B) G protein-coupled receptors in the regulation of cardiovascular system function and the drug target exploration, we summarize the role of these receptors Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Genome-scale CRISPR screening reveals that C3aR signaling is critical for rapid capture receptor (GPCR) that recognizes the complement fragment C3a. and release of small peptide fragments such as C3a, a role for C3aR in macrophage interactions with and uncover a novel and specific role for C3aR in macrophage recognition of fungi." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent This signaling axis was required for effective neutrophil-mediated skin immunity and microbiome homeostasis Activation of Mrgpra2 by defensin triggered neutrophil release of IL-1β and CXCL2 which are vital for proper amplification and propagation of the antibacterial immune response. Read more at the source #DrGPCR #GPCR #IndustryNews

Dopamine receptors are involved in the modulation of fundamental physiological functions, and dysregulation , resolution, or require genetic manipulation. We demonstrate that azodopa activates D1-like receptors in vitro in a light-dependent manner. separating the retinal component of dopaminergic neurotransmission. Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Arrestins interact with G protein-coupled receptors (GPCRs) to stop G protein activation Recent structural studies shed light on the molecular mechanisms involved in GPCR-arrestin coupling, Here, we report the cryo-electron microscopy active structure of the wild-type arginine-vasopressin V2 receptor (V2R) in complex with β-arrestin1. Read more at the source #DrGPCR #GPCR #IndustryNews

Depending on which ligand activates a receptor, it can engage different intracellular transducers. by receptors but by ligand-receptor pairs. However, ligand bias is very complex, making reproducibility and description challenging. The guidelines will aid consistency and clarity, as the basic receptor research and drug discovery communities Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide range of physiological processes. We revealed that AlphaFold2 could capture the overall backbone features of the receptors. reliable high-resolution structural information." Read more at the source #DrGPCR #GPCR #IndustryNews

Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets The adenosine A1 and A2A receptors are expressed in the human brain and have a proposed involvement in Targeting these receptors preclinically can mitigate pathogenic β-amyloid and tau neurotoxicity whilst potential of A1 and A2A receptors. Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "The apelin receptor (APJ) is a target for cardiovascular indications. (Ca2+EC50 = 24 nM, cAMPi EC50 = 6.5 nM) and pharmacokinetic properties (clearance ∼20 mL/min/kg in rats This compound has vastly reduced brain penetration and is devoid of significant off-target liability. Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 " Background and purpose: Vascular tone is regulated by the relative contractile state of Several integrins directly modulate VSMC contraction by regulating calcium influx through L-type voltage-gated roles in vasoregulation. We determined whether SVEP1 and integrin α9β1 can regulate VSMC contraction." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Bone remodeling is precisely regulated mainly by osteoblasts and osteoclasts. Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, little is known about the roles in osteoclasts. But GPR110 knockout and subsequent rescue experiments revealed a pivotal role of GPR110 in the attenuation These results suggest that synaptamide/GPR110 signaling negatively regulates osteoclastogenesis.

August 2022 "GPR21 is an orphan and constitutively active receptor belonging to the superfamily of G-Protein Coupled Receptors (GPCRs). The aim of this study was to evaluate the role of GPR21 in human macrophages, analyzing (i) its involvement in cell migration and cytokine release and (ii) the consequence of its pharmacological inhibition by Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets in Uterine Corpus Endometrial cancer "Adhesion G protein-coupled receptors (adhesion GPCRs), as a member researchers. related to adhesion GPCRs in UCEC." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Oxysterols induce the migration of B-lymphocytes and dendritic cells to interfollicular regions Here, we report the cryo-EM structures of an EBI2-Gi signaling complex with its endogenous agonist 7α These structures reveal an agonist binding site for the oxysterol and a potential ligand entrance site Read more at the source #DrGPCR #GPCR #IndustryNews