October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical Recent advances in X-ray crystallography and cryo-EM have resulted in a wealth of GPCR structures that Here, ensemble refinement (ER) of crystallographic structures is applied to explore the impact of binding of agonists and antagonist/inverse agonists to selected structures of cannabinoid receptor 1 (CB1R), β2 adrenergic receptor (β2 AR) and A2A adenosine receptor (A2A AR). " Read more at the source #DrGPCR

or systemic lipolysis in rat "Introduction: Recurrent hypoglycemia (RH) impairs secretion of counterregulatory Whether and how RH affects responses within metabolically important peripheral organs to counterregulatory Methods: Using a widely adopted rodent model of 3-day recurrent hypoglycemia, we first checked expression The abovementioned studies were repeated in streptozotocin-induced diabetic rat model. Saline-injected rats served as controls." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Case Report of a Juvenile Patient with Autism Spectrum Disorder with a Novel Combination of Copy Number Variants in ADGRL3 (LPHN3) and Two Pseudogenes "We report the finding of two copy number receptor L3 (ADGRL3, former name: latrophilin-3, LPHN3), the other on chromosome 3p26.3 in the region of the two pseudogenes AC090043.1 and RPL23AP39. Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane (GPCR) drug development by displaying subtype selectivity and more specific receptor modulation. Among the allosteric sites known to date, cavities at the receptor-lipid interface represent an uncharacteristic binding location that raises many questions about the ligand interactions and stability, the binding Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Endogenous parathyroid hormone (PTH) and PTH-related peptide (PTHrP) bind to the parathyroid hormone receptor 1 (PTH1R) and activate the stimulatory G-protein (Gs) signaling pathway. bone-resorption effects. presence of PTH or PTHrP at resolutions of 2.8 -4.1 Å. A comparison of the PTH-bound and PTHrP-bound structures reveals distinct ligand-receptor interactions

We summarize recent discoveries that have advanced our understanding of rod outer segment (ROS) morphology and the pathological basis of retinal diseases. We have combined recently published cryo-electron tomography (cryo-ET) data on the ROS with structural Although hypothetical, the reconstruction of the rod phototransduction system highlights the potential ROS discs, suggesting a plausible mechanism by which intrinsic optical signals are generated in the retina

August 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

G protein-coupled receptor 3 (GPR3) belongs to the class A rhodopsin-type GPCR family and is highly expressed However, the potential role of GPR3 in axonal regeneration after neuronal injury has not been elucidated retinal injury in mice. GPR3 was relatively highly expressed in retinal ganglion cells (RGCs). regeneration after ONC in mice."

disease (NAFLD) have yet to be fully delineated and only a single drug, peroxisome proliferator-activated receptor Here, we sought to investigate the role of Regulator of G Protein Signaling 7 (RGS7) in hyperlipidemia-dependent hepatic dysfunction. " Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "G-protein-coupled receptors (GPCR) are present at the cell surface in different conformational However, how these states impact GPCRs biological function and therapeutic targeting remains incompletely Here, we investigated this issue in living cells for the CC chemokine receptor 5 (CCR5), a major receptor These results suggest a link between receptor activation and immobilization. of gp120s. " Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Epithelial tube formation requires Rho1-dependent actomyosin contractility to generate the 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

August 2022 "Background: Activation of signaling effectors by G-protein coupled receptors (GPCRs) depends on different molecular mechanisms triggered by conserved amino acid residues. 7 (TMH7) and the highly conserved NPXXY motif can be subject to different conformational changes in response to biased ligands and could therefore participate in a molecular mechanism to trigger β-arrestin recruitment . " Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, vs. β-arrestin related signaling. biased ligands for the dopamine D1 receptor were reported. We now summarize important pharmacological, molecular, and cellular studies relevant to D1-mediated β-arrestin-related Read more at the source #DrGPCR #GPCR #IndustryNews

Nanobody binding stabilizes G-protein-coupled receptors (GPCR) in a fully active state and modulates However, the atomic-level basis for this allosteric regulation remains elusive. Besides, ligand-specific subtle differences in the conformations assumed by intracellular loop 2 and extracellular loop 2 are captured from the trajectories of various ligand-bound receptors in the presence Read full article

therapy but the disease recurs as incurable castration-resistant prostate cancer (CRPC), requiring new We previously demonstrated that the G protein-coupled receptor (GPCR) arginine vasopressin receptor type1A AVPR1A is part of a family of GPCR's including arginine vasopressin receptor type 2 (AVPR2). vasopressin receptors, and knockout of AVP in CRPC cells significantly reduced proliferation suggesting These data indicate that the AVP/arginine vasopressin receptor signaling axis represents a promising

September 2022 Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent Thrombus Formation under Shear "Glycoprotein (GP)VI and integrin αIIbβ3 are key signaling receptors kinase 2, PTK2), the shear-dependent collagen receptor GPR56 (ADGRG1 gene), and calcium and integrin-binding The suppressive rather than activating effects of pGRP were confined to blood flow at a high shear rate Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Introduction Protease activated receptors 1 (PAR1) and 4 (PAR4) agonists are used to Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Recent studies revealed butyrate and secondary bile acids, produced by the intestinal microbiome, potentiate RNA sequencing of intestinal epithelial cells responding to butyrate and secondary bile acids in combination sequencing findings and discovered a role for intestinal HNF4α in P-gp regulation. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs Interestingly, RGS (Regulators of G protein signaling) proteins, which negatively regulate GPCR signaling Considering this, we investigated the role of RGS20 as a potential prognostic marker in 28 different Our analysis further supports the putative function of RGS proteins, particularly RGS20, in cancer." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Ginsenoside Rg5 allosterically interacts with P2RY12 and ameliorates deep venous thrombosis by counteracting neutrophil NETosis and inflammatory response "Deep venous thrombosis (DVT) highly occurs DVT formation is a time-dependent inflammatory process in which NETosis plays an important role. However, whether ginsenoside Rg5 from species of Panax genus could alleviate DVT and its underlying mechanism Read more at the source #DrGPCR #GPCR #IndustryNews

The bioactive lysophospholipid sphingosine-1-phosphate (S1P) acts via five different subtypes of S1P receptors S1P5 is predominantly expressed in nervous and immune systems, regulating the egress of natural killer In this article, we describe a 2.2 Å resolution room temperature crystal structure of the human S1P5 relationship data. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started Although the high-resolution crystal structures of the DOR with both agonist and antagonist have recently been solved, the activation mechanism remains to be elusive. The putative key residues (W274, D95, V267, L139, V263, M142, T260, R146, R258 and others) involving Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "The follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs). FSHR is involved in reproductive processes such as gonadal development and maturation. (HR), is characteristic for these receptors. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Research on cancer therapies focuses on processes such as angiogenesis, cell signaling , stemness, metastasis, and drug resistance and inflammation, all of which are influenced by the cellular techniques, have been tested to reduce the malignancy and generate a harmful microenvironment for the In 2008 (and for the first time in the clinic), the therapeutic benefits of the β-adrenergic receptor Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Angiotensin-(1-7) improves cognitive function and reduces inflammation in mice following Angiotensin 1-7 (Ang-1-7), an endogenous peptide, acts at the G protein coupled MAS1 receptors (MASR) to inhibit inflammatory mediators and decrease reactive oxygen species within the CNS. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative to its N-terminal fragment 1 to 36 "The parathyroid hormone (PTH)-related protein (PTHrP) is indispensable activation, (ii) receptor signaling via Gs and Gq, and (iii) receptor internalization and recycling cAMP signaling from the plasma membrane and fails to stimulate iCa2+ release and recruit β-arrestin. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Serotonin receptor 5-HT2A and tropomyosin receptor kinase B (TrkB) strongly contribute A blockade of 5-HT2A receptor with the preferential antagonist ketanserin prevented the receptor-mediated downregulation of TrkB phosphorylation without restoring the TrkB response to its agonist 7,8-DHF in An expression analysis revealed strong developmental regulation of 5-HT2A and TrkB expressions in the Our data reveal the functional role of 5-HT2A–TrkB receptor heterodimerization and suggest that the regulated

September 2022 Sweet taste receptor agonists attenuate macrophage IL‐1β expression and eosinophilic inflammation chronic rhinosinusitis (CRS) and considered a major therapeutic target. Autophagy deficiency in myeloid cells plays a causal role in eosinophilic CRS (ECRS) via macrophage IL ‐1β overproduction, thereby suggesting autophagy regulation as a potential therapeutic modality. Read more at the source #DrGPCR #GPCR #IndustryNews