Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for metabolic protein-coupled receptors (GPCRs) are a large family of cell surface receptors that are the targets for many central to appropriate glucose homeostasis through their secretion of insulin, and islet function can be modified altered under pathophysiological conditions and, in this review, we have compared expression of GPCR mRNAs

These receptors are the most clinically productive drug targets at present. Despite decades of research on the signaling consequences of molecule-receptor interactions, conformational Using bioluminescence resonance energy transfer -based biosensors, second messenger assays, and biochemical This single point mutation in extracellular loop 2 of the β 2AR is sufficient to intrinsically bias the We characterized the effects of extracellular loop mutations on agonist-promoted interactions of GPCRs

programming packages for cheminformatics and structural bioinformatics are powerful tools to build modular TeachOpenCADD is a teaching platform developed by students for students, which provides teaching material offered, using open source packages such as the Python packages rdkit, pypdb, biopandas, nglview, and mdanalysis Beyond their teaching purpose, the TeachOpenCADD material can serve as starting point for users’ project-directed modifications and extensions.

Glioma is the most common adult malignant brain tumor and requires novel therapeutic strategies to improve Moreover, through systematic survival analysis on OR genes, OR51E1 (mouse Olfr558) was identified as In addition to transcriptomic analysis, mutational profiles revealed that somatic mutations in OR genes OR5D18 (mouse Olfr1155) was the most frequently mutated OR gene, and OR5AR1 (mouse Olfr1019) showed IDH wild-type-specific mutation.

Current progress in our knowledge of the itch processing, the numerous mediators and receptors involved Currently, inhibitors of IL-31, IL-4/13, NK1 receptors, opioids and cannabinoids, JAK, PDE4 or TRP are the main However, many new targets, such as Mas-related GPCRs and unexpected new pathways need to be also explored

nanoparticles in the range of μg/L in C. elegans The aim of this study was to identify Gα proteins mediating Caenorhabditis elegans was used as an animal model, and both gene expression and functional analysis Moreover, GOA-1 acted upstream of MPK-1/ERK MAPK, JNK-1/JNK MAPK, DBL-1/TGF-β, and DAF-7/ TGF-β, GSA- 1 functioned upstream of MPK-1/ERK MAPK, JNK-1/JNK MAPK, and DBL-1/TGF-β, and GPA-10 functioned upstream Therefore, neuronal Gα proteins of GOA-1, GSA-1, and GPA-10 functioned to transduce signals of multiple

SEPTEMBER 26-29, 2022 (Leipzig, Germany)​ 4GPCRnet meeting bringing together four of the biggest GPCR networks in Europe for a joint meeting in Leipzig. and ERNEST plus DFG-funded CRC1423 and RU2372 ) have joined forces to organize an international meeting The event will take place in the heart of Leipzig, which offers a colorful mixture of culture and vivid

SNOWBIRD RESORT, UTAH, UNITED STATES The superfamily of G protein-coupled receptors (GPCRs) act as molecular to respond to a highly diverse range of chemical stimuli, they represent the therapeutic targets for many While GPCRs are considered a well-established field, recent technological advances to dissect the molecular mechanisms of GPCR function has revealed new paradigms with increasingly complex models of receptor The goal of this meeting is to bring together a highly interdisciplinary group of scientists to exchange

therapeutic antibodies against G protein-coupled receptors (GPCR) identified by Sosei Heptares . " Read more

While vaccine-makers race to test their shots against the variant, the monoclonal antibody sotrovimab Sotrovimab is the first monoclonal antibody showing preclinical efficacy against all COVID-19 variants , including the delta and omicron mutations, Vir CEO George Scangos said on a Dec. 7 call with analysts Read more at the source #DrGPCR #GPCR #IndustryNews

applied with the goal of enabling the discovery of novel therapeutic antibody drug candidates. " Read more

Drug Candidates and Leads Against 10 Oncology Targets – Radionetics and Crinetics to Collaborate on Multiple Read more at the source #DrGPCR #GPCR #IndustryNews

company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs) with a novel drug modality , proven discovery platform and best-in-class molecules, today announced the successful completion of The CCL2/CCR2 pathway plays an important role in oncology, inflammatory, metabolic, and neurological Read more at the source #DrGPCR #GPCR #IndustryNews

Sharing how she became a scientist, educator, mentor, and the powerhouse we know today.

Therapeutics (SIX: ADXN and Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based ADX71149 is a selective metabotropic glutamate type 2 (mGlu2) receptor positive allosteric modulator to be included in a potential global development of ADX71149 for the treatment of epilepsy. " Read more

Nasdaq: TRVN), a biopharmaceutical company focused on the development and commercialization of novel medicines Read more at the source #DrGPCR #GPCR #IndustryNews

This $60,000 grant from Diabetes Research WA will assist the Perkins' Molecular Endocrinology and Pharmacology Read more at the source #DrGPCR #GPCR #IndustryNews

2021 Positive Recommendation for Use of TAVNEOS™ (avacopan) in ANCA Vasculitis Adopted by European Medicines Agency (EMA) Committee for Medicinal Products for Human Use (CHMP) "SAN CARLOS, Calif. , Nov. 12, 2021 (GLOBE NEWSWIRE) -- ChemoCentryx , Inc. , (Nasdaq: CCXI), today announced that the European Medicines polyangiitis (MPA)." Read more at the source #DrGPCR #GPCR #IndustryNews

proud and grateful to receive honorary doctorate yesterday from Karolinska Institute and celebrate with my Read more at the source #DrGPCR #GPCR #IndustryNews

structure-based technology has passed a key test, in enabling the discovery of orally available small molecules aimed at intractable and poorly drugged membrane and complex-bound protein targets. Read more at the source #DrGPCR #GPCR #IndustryNews

The vision is to develop novel muscarinic receptor agonists for schizophrenia and other neuropsychiatric Neurocrine Biosciences anticipates initiating a Phase 2 study with the selective M4 agonist HTL-0016878 in schizophrenia in 2022 and Phase 1 studies for a dual M1/M4 and selective M1 agonist in 2023." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 "Target class-specific libraries mean you need to screen less to identify high-quality As a result, most approved library-derived antibodies originate from just three libraries. To target hard-to-drug targets like G protein-coupled receptors (GPCRs), more libraries, including better and more targeted libraries, are needed." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 " Chronic use of most opioids causes tolerance; the new compounds avoid this and other at Scripps Research in Florida have created a collection of new pain-relieving compounds that, like morphine and other drugs, provide relief via activation of opioid receptors, but without inducing many dangerous Read more at the source #DrGPCR #GPCR #IndustryNews

unknown, and there is no ideal drug for the specific treatment of pSS. β-arrestin2 is a key protein that mediates receptors (GPCRs) and it participates in inflammatory and immune responses that have been found to mediate In this study, we established an experimental Sjögren's syndrome (ESS) mouse model to elucidate the molecular mechanisms of β-arrestin2 in pSS. increased saliva flow, alleviated salivary gland indices, and improved tissue integrity in the ESS model

Come attend this month's virtual café talk to see the awesome work of Dr. Stuart Maudsley on how an aging physiological context affects #GPCR signaling #drgpcr.

Don’t miss out on episode 50 of the Dr. GPCR podcast! Give it a listen to hear from Dr. Thomas P. Sakmar on how the molecular studies of rhodopsin paved the way to understanding #GPCRs Be sure to subscribe