August 2022 "Host response to infection involves the activation of the complement system leading to the Complement factor C5a exerts its effect through the activation of C5aR1, chemotactic receptor 1, and Here, we discuss recent crystal structures of inactive C5aR1 in terms of an inverted orientation of helix By comparing two C5aR receptors C5aR1 and C5aR2 we explained differences between their signaling pathways Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "G-protein-coupled receptors (GPCRs) receive signals from ligands with different efficacies Previous studies revealed how ligands with different efficacies activate GPCRs. We report the cryo-EM structures of β1-adrenergic receptor (β1-AR) in complex with Gs (GαsGβ1Gγ2) and β1-AR to the cAMP response initiated by the three different ligands, with residue-specific functional Read more at the source #DrGPCR #GPCR #IndustryNews

cryogenic-electron microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors However, applying it to GPCRs without signaling proteins remains challenging because most receptors lack exploring different fusion protein designs, which lead to structures of antagonist bound A2A adenosine receptor at 3.4 Å resolution and unliganded Smoothened at 3.7 Å resolution. Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) in the central nervous system, which mediates the functional response to endocannabinoids and Cannabis New high-resolution structures of CB1 receptor in different functional states have significantly improved In this review, we describe the structural determinants for modulation of CB1 receptors by different types of ligands, as well as the differences between CB1 and its homologous, the CB2 receptor.

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. The scope of our review is to present the most important of the aforementioned ligands, highlight their Read more at the source #DrGPCR #GPCR #IndustryNews

November 2 - 4: We are sponsoring the GPCR Retreat and look forward to seeing you there! Phase 1/2 study of sorafenib added to cladribine, high-dose cytarabine, G-CSF, and mitoxantrone in untreated in GPCRs as Drug Targets: Allosteric Function and Biased Signaling" at the DOT NEW October 2 - 3, 2023 production to candidate validation October 25 - 27, 2023 | 3rd Annual Meeting IRN I-GPCRNet November 2 May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2

and cones rely on unique Gγ1 ( Gngt1 ) and Gγc ( Gngt2 ) isoforms, respectively. To determine whether Gγ1 regulates uniquely rod phototransduction, we generated transgenic rods expressing rod cells and restoration of Gαt1 expression, which is greatly reduced in Gγ1-deficient rods. Recordings from individual transgenic rods showed that photosensitivity impaired in Gγ1-deficient rods Consistent with this, transretinal ERG recordings revealed gradual response recovery in moderate background

September 2022 Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1 ) and its interactions with antagonist and agonist ligands "The CX3C chemokine receptor 1 (CX3CR1), a member of the class A of G Protein-Coupled Receptors (GPCR) superfamily, and its ligand fractalkine We analyzed the receptor conformational changes and described interactions within its key regions and Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Receptor-activity-modifying proteins (RAMPs) are ubiquitously expressed membrane proteins However, it is unknown whether and how RAMP proteins may affect PTH1R function. Additionally, RAMP2 increases both PTH- and PTHrP-triggered β-arrestin2 recruitment to PTH1R. These data uncover a critical role of RAMPs in the activation and signaling of a GPCR that may provide Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "G protein-coupled receptors (GPCRs) are signaling hubs in cell membranes that regulate Our results show that the short-term diffusion coefficient of the receptor decreases upon cholesterol Analysis of SPT trajectories revealed that relative populations of receptors undergoing various modes These results are supported by our recent work and present observations that show polymerization of G-actin Taken together, our results bring out the interdependence of cholesterol and actin cytoskeleton in regulating

The G-protein–coupled receptor pathway is inhibited by the regulator of G-protein signaling (RGS) Sst2 G-protein signaling activates the MAPK Fus3, which phosphorylates the RGS; however, the role of this We found that pheromone-induced RGS phosphorylation peaks early; the phospho-state of RGS controls its We found that RGS complexes with Kel1 and prefers the unphosphorylatable RGS mutant. are rescued by overexpression of Kel1.

September 2022 GASP1 enhances malignant phenotypes of breast cancer cells and decreases their response cycle with IGF1/IGF1R signaling pathway "There is a potential correlation between G-protein-coupled receptor-associated Mechanistically, GASP1 inhibited proteasomal degradation of insulin-like growth factor 1 receptor (IGF1R its downstream signaling pathways such as NF-κB, PI3K/AKT, and MAPK/ERK pathways given their critical roles Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under Transcript and protein levels were determined by RT-qPCR and Western blot, respectively. Downregulation of the A2B receptor decreases MRP3 expression and chemosensibilizes GSCs treated with These data suggest that hypoxia-dependent activation of A2B adenosine receptor promotes survival of GSCs Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Identification and functional characterization of the sulfakinin and sulfakinin receptor However, there is no report on the functional role of SK in the Chinese white pine beetle, Dendroctonus Additionally, RNA-interference (RNAi) using double-stranded RNA to knock down SK and SKR reduced the The results show that the SK signal pathway plays a positive and significant role in feeding regulation Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "T cells are master regulators of the immune response tuning, among others, B cells, macrophages To exert their functions requiring high sensibility and specificity, T cells need to integrate different for the proper and efficient response of these cells to distinct triggers. activation, focusing on the role of CD28, chemokine receptors and the actin cytoskeleton. Read more at the source #DrGPCR #GPCR #IndustryNews

of C3 cleavage, which interacts with membrane-bound receptor C3aR to regulate innate immune cell function Specifically, previous research has identified mechanistically distinct and cell type–specific roles Historically, the production of C3a has been relegated to the serum; however, recent studies have provided In light of these new results, it is imperative that we revisit previous studies regarding the role of Thus, this review will cover specific roles of C3aR in driving cell type–specific and tissue specific

September 2022 "The glucagon-like peptide-1 receptor (GLP-1R) plays a key role in metabolism and is an Recent studies in experimental animals have shown that certain subsets of T cells express functional GLP-1R, indicating an immune regulatory role of GLP-1. the high induction of GLP-1R in human iTreg cells, we hypothesize that GLP-1R+ iTreg cells play a key role Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "The human sweet taste receptor is a heterodimeric receptor composed of two distinct G-protein-coupled receptors (GPCRs), TAS1R2 and TAS1R3. region (CRR). /TAS1R3 receptor. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Divergent roles for the gut intraepithelial lymphocyte GLP-1R in control of metabolism lymphocytes (IELs) are thought to calibrate glucagon-like peptide 1 (GLP-1) bioavailability, thereby regulating Here, we show that the gut IEL GLP-1 receptor (GLP-1R) is not required for enteroendocrine L cell GLP These data reposition key roles of the L cell-gut IEL GLP-1R axis, revealing mechanisms linking GLP-1R Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "The endocannabinoid system plays a key role in the intersection of the nervous, endocrine , and immune systems, regulating not only their functions but also how they interplay with each other Endogenous ligands, named endocannabinoids, are produced “on demand” to finely regulate the synthesis and secretion of hormones and neurotransmitters, as well as to regulate the production of cytokines Read more at the source #DrGPCR #GPCR #IndustryNews

, such as the prokineticin receptors, and regulates energy expenditure and appetite. The aim of this work was to analyze the functional role of the specific arginine residue at position Results obtained with the MRAP2 mutants R125H and R125C, which are found in human patients with extreme Understanding the mechanism by which MRAP2 regulates G protein-coupled receptors helps in elucidating Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Epithelial tube formation requires Rho1-dependent actomyosin contractility to generate Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. 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 We also report on unexpected Fog-independent roles for Smog in maintaining epithelial integrity and organizing

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous Moreover, whether the receptor can also couple to Gs , Gq/11 and G12/13 is unclear. The results show that the GPR15 receptor preferentially couples to Gi/o rather than other pathways in and the activation rate is significantly slower. 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 The interaction of arrestins with GPCRs requires both agonist activation and receptor phosphorylation stable receptor-arrestin complexes." Read more at the source #DrGPCR #GPCR #IndustryNews

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 Our results suggest that strategies to selectively target OGR1 expression may represent a novel therapeutic Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "The activation of phospholipase C (PLC) is thought to have a key role in the cardiomyocyte response to several different hypertrophic agents such as norepinephrine, angiotensin II and endothelin PLC activity results in the generation of diacylglycerol and inositol trisphosphate, which are downstream In this article, we describe the signal transduction elements that regulate PLC gene expression. Read more at the source #DrGPCR #GPCR #IndustryNews

🥁 Drum rolls, please! Our guest is the wonderful Dr. Rosie Dawaliby! GPCR Ecosystem paid membership ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ep-84-with-rosie-dawaliby

Each ADS represents six shares. Read more at the source #DrGPCR #GPCR #IndustryNews