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Get ready for an expedition, GPCR explorers! Welcome back to your weekly GPCR quest! Thank you to all participants in Dr. Terry Kenakin's educational initiative this fall! Classified GPCR News  Let’s dive into the   Classified GPCR News from October 21st to 27th, 2024 Industry Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and

AlphaFold, homology modeling was the most common method for predicting G protein-coupled receptor (GPCR similarity to available templates, homology models tend to be less accurate, a notable challenge for GPCRs GPCRs are dynamic, switching between multiple conformations, and many have only distant homologs with The introduction of AlphaFold2 marked a major advancement in the field of GPCR structure prediction. While AlphaFold2’s ability to predict static structures was groundbreaking, however, GPCRs are highly

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network located on intracellular loop 2 that is subject to RNA editing, which differentially affects GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

that the affinity of Fzd for Dvl was not affected by Wnt ligands, in contrast to other members of the GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR 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 the GPCR-β-arrestin complex. However, whether β-arrestin1 and 2 respond differently for binding to the same GPCR is still unknown. Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter

Human cells express over 800 G-protein-coupled receptors (GPCRs) to facilitate communication with the Capturing the dynamics of GPCR activation has always been a challenge because G protein activation in With this high-resolution, dynamic view of GPCR activation, scientists can better tackle diseases by Beyond GPCRs, the methods and insights from this study can be applied to other fast, transient biological Time-resolved cryo-EM of G-protein activation by a GPCR. Nature (2024).

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

February 2022 Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with Better known as GPCR, the fruitful research space has led to more than 700 approved drugs over previous The company's co-founder, GPCR pioneer and Nobel laureate Robert Lefkowitz, M.D., has 50 years of experience Read more at the source #DrGPCR #GPCR #IndustryNews

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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

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

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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

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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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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 entered a strategic research collaboration to identify and validate novel G protein-coupled receptor (GPCR drug discovery programs in the area of gastrointestinal diseases. " Read more at the source #DrGPCR #GPCR

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

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Introduction Dopamine receptors are G-protein-coupled receptors (GPCRs), which have 5 subtypes -D1-5. Fluorescence anisotropy (FA) assay has been used to study the ligand binding kinetics of many GPCRs.[ Miniaturization is key for HTS application, so achieving good Z’ values for GPCR ligand binding assays Altogether, the development of similar probes for other GPCRs and further development of measurement How the Dynamic Properties and Functional Mechanisms of GPCRs Are Modulated by Their Coupling to the

November 2021 Dr. Kevin Pfleger and Dr. "Congratulations to Perkins Professor Kevin Pfleger and Dr Elizabeth Johnstone who were awarded one of Read more at the source #DrGPCR #GPCR #IndustryNews