September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Proton-sensing G-protein coupled receptors are activated by acidic environments, but their role in fibrosis Here, we report that the Ovarian Cancer G-Protein Coupled Receptor1 (OGR1 or GPR68) has dual roles in We demonstrate that OGR1 protein expression is significantly reduced in lung tissue from patients with Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid The primary analgesic target of opioids is the μ-opioid receptor (MOR). receptor. Finally, inhibition of Gq-GPCR coupling in mice enhanced the antinociceptive effects of morphine. that would allow for lower dose utilization of opioid analgesics. " Read more at the source #DrGPCR #GPCR

August 2022 "Histamine exerts its physiological functions through its four receptor subtypes. In this work, we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled receptor (GPCR), which is expressed in a wide variety of cell and tissue types. At the same time, H2R as a GPCR imparts many unresolved questions, such as the functional relevance of Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), This article focuses on the role of Aβ granules and their possible interaction with GPCRs that modulate Read more at the source #DrGPCR #GPCR #IndustryNews

G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular effector proteins. Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase However, the rank order of the agonists for G protein- and GRK2-M3R interaction was the same, suggesting that G protein and GRK2 binding to M3R requires similar receptor conformations, whereas requirements

May 2022 "Seoul, South Korea, 28 April 2022 – GPCR therapeutics , Inc., a venture-backed clinical stage international biopharmaceutical company with an innovative approach to drug discovery based on targeting G Protein Coupled Receptors (GPCR) pairs, today announced four appointments to its Scientific Advisory GPCR just had a very successful first meeting including all the Scientific Advisory Board." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Design and validation of recombinant protein standards for quantitative Western blot analysis protein-coupled receptor (GPCR) levels requires the use of purified protein standards containing the GPCRs in general and cannabinoid CB1 receptor in particular show a progressive tendency to aggregate Results: Here we generated highly soluble and stable recombinant protein constructs GST-CB1414-472 and 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 , associated with an original V2R/β-arrestin1 interface involving all receptor intracellular loops. Read more at the source #DrGPCR #GPCR #IndustryNews

avoid a prolonged pro-inflammatory neutrophil response, signaling downstream of an agonist-activated G protein-coupled receptor (GPCR) has to be rapidly terminated. Among the family of GPCR kinases (GRKs) that regulate receptor phosphorylation and signaling termination The medium chain fatty acid receptor GPR84 as well as formyl peptide receptor 2 (FPR2), receptors expressed analysis of subcellular fractions revealed a cytosolic localization. " Read more at the source #DrGPCR #GPCR

Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, GPR110 belongs to adhesion GPCR and was the functional receptor of N-docosahexaenoyl ethanolamine (also Synaptamide suppressed osteoclastogenesis induced by receptor activator of nuclear factor-kappa B ligand Read more at the source #DrGPCR #GPCR #IndustryNews

Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. During Drosophila embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog The SG receptor that transduces the Fog signal into Rho1-dependent myosin activation has not been identified Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin Read more at the source #DrGPCR #GPCR #IndustryNews

ligands "G-protein coupled receptors (GPCRs) have been largely targeted in a wide range of diseases, We selected the adenosine receptor 2B (A2BAR), specifically expressed in cancer cell lines compared with Fluorescent probes allowed semi-quantitative receptor mapping in living cells and validated the specific As well, fluorescent ligands were effective at monitoring real-time A2BAR receptor labeling using live-imaging 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 activation by glucagon within 5 min and transit via EEA1-marked endosomes shown previously to be sites of GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

: Analysis of Diffusion Modes "G protein-coupled receptors (GPCRs) are signaling hubs in cell membranes Serotonin1A receptors are important members of the GPCR family and are implicated in neuropsychiatric To explore the role of cholesterol in lateral dynamics of GPCRs, we utilized single particle tracking results bring out the interdependence of cholesterol and actin cytoskeleton in regulating diffusion of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Opioid receptors (ORs) represent one of the most significant groups of G-protein coupled receptor (GPCR) drug targets and also act as prototypical models for GPCR function. Read more at the source #DrGPCR #GPCR #IndustryNews

of Adhesion Receptor GPR97 "Adhesion G-protein-coupled receptors (aGPCRs)-a major family of GPCRs-play The orphan receptor GPR97, activated by glucocorticoid stress hormones, is a prototypical aGPCR. only allosterically strengthens the internal interactions between Gαo and Gβγ, but also enhances the coupling of the Go protein, and offers guidance for future drug design of aGPCRs." Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 Confo Therapeutics receives €1.7 million VLAIO grant for further research on GPCR modulators The grant should help expand Confo Therapeutic ’s research on G protein-coupled receptor (GPCR) drug candidates. " Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal mast cells "A novel mast cell-specific G-protein-coupled receptor (GPCR), known as Mas-related G protein-coupled receptor-B2 (MRGPRB2), plays important roles in immune response. Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of Cannabinoid CB1 Receptor Bound to a Negative Allosteric Modulator, ORG27569, and Analogs "A growing number of G-protein-coupled receptor (GPCR) structures reveal novel transmembrane lipid-exposed in the access and binding of ORG27569 and its analogs at the transmembrane site of cannabinoid CB1 receptor Read more at the source #DrGPCR #GPCR #IndustryNews

protein-coupled receptors in the oriental fruit moth Grapholita molesta The oriental fruit moth Grapholita Neuropeptides and their specific receptors (primarily G protein-coupled receptors, GPCRs) regulate multiple A total of 41 neuropeptide GPCR genes belonging to three classes were also identified. These GPCRs and their probable ligands were predicted. to determine physiological functions and pharmacological characterization of neuropeptides and their GPCRs

September 2022 "Class A (rhodopsin-like) G protein-coupled receptors (GPCRs) are constitutive phospholipid scrambling is not detectable in the resting plasma membrane of mammalian cells that is replete with GPCRs GPCRs to scramble lipids. This mechanism may explain the inability of GPCRs to scramble lipids at the plasma membrane." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "G-protein-coupled receptors (GPCRs) receive signals from ligands with different efficacies , and transduce to heterotrimeric G-proteins to generate different degrees of physiological responses Here, we investigate how a GPCR activates G-proteins upon binding ligands with different efficacies. We report the cryo-EM structures of β1-adrenergic receptor (β1-AR) in complex with Gs (GαsGβ1Gγ2) and These data provide insights into the ligand efficacy in the activation of GPCRs and G-proteins."

hypercalcemia caused by biased allosteric CaSR autoantibodies "Biased agonism is a frontier field in GPCR Acquired hypocalciuric hypercalcemia (AHH) is a rare disease caused by calcium-sensing receptor (CaSR This emphasizes the importance of the Gi/o (pertussis toxin-sensitive G proteins, whose βγ subunits activate of AHH and the mechanisms by which the biased agonism of GPCRs operate." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "G-protein-coupled receptors (GPCRs) are involved in a wide array of physiological and In addition, the molecular mechanisms underlying GPCR-induced post-translational signaling regulation Here, we find that protease-activated receptor 4 (PAR4) unexpectedly acts as a potent oncogene, inducing Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 " Background and purpose: The interaction of arrestins with G-protein coupled receptors (GPCRs) desensitizes agonist-dependent receptor responses and often leads to receptor internalization GPCRs that internalize without arrestin have been classified as "class A" GPCRs whereas "class B" GPCRs The interaction of arrestins with GPCRs requires both agonist activation and receptor phosphorylation Read more at the source #DrGPCR #GPCR #IndustryNews

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 , and several allosteric modulators of this GPCR have been evaluated in clinical trials. Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

October 2022 β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR in living cells "β-arrestins mediate regulatory processes for over 800 different G protein-coupled receptors (GPCRs) by adopting specific conformations that result from the geometry of Here, we show differences between conformational changes that are induced by P-R* or R* receptor states and further disclose the impact of site-specific GPCR phosphorylation on arrestin-coupling and function

September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization evidence that distal carboxyl-terminal tail (C-tail), but not proximal, phosphorylation of the chemokine receptor We demonstrate by pharmacologic inhibition of GRK2/3-mediated phosphorylation of the chemokine receptor CXCR4 coupled with site-directed mutagenesis and bioluminescence resonance energy transfer approaches that distal, not proximal, C-tail phosphorylation sites are required for recruitment of the adaptor protein