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October 2022 "Understanding the activation of G protein-coupled receptors (GPCRs) is of paramount importance Although many cardiovascular GPCRs have been extensively studied as model receptors for decades, new As a result, there is an ongoing need to develop novel approaches to monitor and to modulate GPCR activation nanobodies have been adopted to elucidate the structure, pharmacology, and signaling of cardiovascular GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

2022 Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR the Sosei Heptares compound library for its industry-leading biology platform to identify potential GPCR City-based Kallyope, pioneers in drug discovery involving the gut-brain axis, have entered a strategic research collaboration to identify and validate novel G protein-coupled receptor (GPCR) targets with a goal of drug discovery programs in the area of gastrointestinal diseases. " Read more at the source #DrGPCR #GPCR

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release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled receptors (GPCRs In this review, we discuss important aspects of adrenal GPCR signaling and regulation, as they pertain modulation of cardiac function in the context of chronic HF, by focusing on the 2 best studied adrenal GPCR the β-arrestins in the adrenals, 2 protein families that regulate the signaling and functioning of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

are small-lipidated peptides designed from the intracellular loops of G protein-coupled receptors (GPCRs ) that act in an allosteric manner to modulate the activity of GPCRs. the past 2 decades, pepducins have progressed initially from pharmacologic tools used to manipulate GPCR To date, pepducins designed from numerous GPCRs have been studied for their impact on pathologic conditions Read more at the source #DrGPCR #GPCR #IndustryNews

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transcription is endocytosis-dependent in primary hepatocytes "A number of G protein-coupled receptors (GPCRs 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

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August 2022 "The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) in Guided Pharmacology of Membrane Proteins (BJP 75th Anniversary). " Read more at the source #DrGPCR #GPCR

November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures The method has found druggable sites overlapping with the cocrystallized allosteric ligands in 21 GPCR 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 Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

Hi GPCR lovers👋, Ready for exciting news in the GPCR world? Read them below! GPCR News, please subscribe to our monthly newsletter. GPCR Activation and Signaling The adhesion GPCRs CELSR1-3 and LPHN3 engage G proteins via distinct activation 2 - 4, 2023) GPCR Jobs NEW Associate Director / Director, Clinical Operations Postdoctoral Research GPCR Ecosystem

Notably, G-protein-coupled receptors (GPCRs), representing the biggest drug target, have been revealed Historically, drug discovery efforts targeting GPCRs focused on G-protein-dependent signaling pathways Recent research has unveiled the emergence of G-protein-independent pathways, particularly those involving By understanding the intricacies of GPCR signaling and utilising advanced assay technologies, researchers Minireview: targeting GPCR activated ERK pathways for drug discovery.

August 2022 RAB-Symposium - Regulatory Autoantibodies Targeting GPCRs. September 15-16, 2022. GPCRs are involved in a variety of physiological and pathophysiological processes. So far, numerous therapeutics targeting GPCRs have been developed, with a focus on small molecules and Recently, functional autoantibodies targeting GPCRs have been associated with various disease-specific Read more at the source #DrGPCR #GPCR #IndustryNews

November 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed treatment of psychiatric and neurodegenerative diseases, and several allosteric modulators of this GPCR libraries have complementary advantages and illustrate how access to high-resolution structures of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

Hi GPCR lovers! Stay tuned for the latest buzz on GPCRs. Conference Simon Bekker-Jensen and Mette M Rosenkilde received two proof of concept grants from European Research , Medical Affairs Associate Scientist - Technology Senior Research Scientist/Principal Scientist- Technology Tissue Culture Scientist/Tissue Culture Manager Postdoctoral Researcher Director - Targeted Oncology Senior Scientist - Antibody Engineering Scientist—Immuno-Oncology Convergent Research - Senior Scientist

Originally, β-arrestins were identified for their contribution to GPCR desensitization to agonist-mediated However, current investigations have now recognized that in addition to GPCR arresting (hence the name Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

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The interpretation of high and low affinity binding sites  on GPCRs.   Unlock “Rethinking Affinity” Now Only in Terry's Corner _____ #GPCR #BindingAffinity #Pharmacology

lipids have been shown to stabilize an active conformation of class A G-protein coupled receptors (GPCRs ) through a conserved binding site, not present in class B GPCRs. For class B GPCRs, previous molecular dynamics (MD) simulation studies have shown PI(4,5)P2 interacting conformation of GCGR through a binding site conserved across class B GPCRs but absent in class A GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR Virtual Cafe? Join us for another virtual cafe talk to hear about the amazing work that Dr. Simone Promel / Promel Lab is doing on adhesion #GPCRs. Register here (free): https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #podcast

October 2022 "While the role of G-protein-coupled receptors (GPCR) in cancer is acknowledged, their underlying Protease-activated receptors (PAR), a subgroup of GPCRs, form a family of four members (PAR1-4) centrally Read more at the source #DrGPCR #GPCR #IndustryNews

Hello Readers👋, Welcome to our GPCR weekly newsletter! GPCRs in Neuroscience Physiological Condition-Dependent Changes in Ciliary GPCR Localization in the Brain drug discovery - Design Pharmaceuticals Call for GPCR Papers GPCRs: Signal Transduction. GPCR Events, Meetings, and Webinars NEW 4th ERNEST GPCR ECI zoominar. GPCR Ecosystem

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GPCR Symposium event held on March 24th? GPCR Activation and Signaling Autoregulation of GPCR signalling through the third intracellular loop. Papers GPCRs: Signal Transduction. GPCR Events, Meetings, and Webinars GEM2023. (March 14-17, 2023). GPCR Ecosystem

August 2022 "GPCRs in Medicinal Chemistry Event 8th RSC / SCI symposium on GPCRs in Medicinal Chemistry 6th September 30th September – online registration (card payments)" Read more at the source #DrGPCR #GPCR

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). Read more at the source #DrGPCR #GPCR #IndustryNews

Get ready to stay up-to-date with the latest research, advancements, and news in the field. Bioinformatics/Data Science at Department of Drug Design and Pharmacology Scientist/Senior Scientist (Research Biochemistry) Speculative Applications (Mass Spectrometry) Speculative Applications (Chemistry) Post-Doctoral Research Assistant Research Fellow - School of Physics and Astronomy Postdoctoral Research Associate (Fixed Term GPCR Ecosystem

sweet taste receptor is a heterodimeric receptor composed of two distinct G-protein-coupled receptors (GPCRs The TAS1R2 and TAS1R3 subunits are members of a small family of class C GPCRs whose members share the Read more at the source #DrGPCR #GPCR #IndustryNews

"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