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Provided by 5AM and Frazier – Pipeline is Built from Crinetics’ Core Nonpeptide Platform and Includes Drug Read more at the source #DrGPCR #GPCR #IndustryNews

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ADXN and Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based drug potential global development of ADX71149 for the treatment of epilepsy. " Read more at the source #DrGPCR #GPCR

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GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry ll gain: Why saturation and displacement assays fail when protein stoichiometry shifts How two-stage GPCR Proper orthosteric binding design prevents those errors before they propagate into SAR narratives. Complex Two-Stage Biology Behind Orthosteric Binding GPCR pharmacology rarely follows the neat Langmuir Clues that point to true multiple-site binding rather than two-stage GPCR biology: Disrupting G protein

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GPCRs represent major drug targets, as indicated by the fact that about 40% of all drugs currently used in clinical practice mediate their therapeutic effects by acting on GPCRs. Like many other organs, various GPCRs play a role in regulating liver function. It is predicted that more than 50 GPCRs are expressed in the liver. cells that regulate liver fibrosis, may lead to the development of drugs that can improve hepatic fibrosis

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

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One such platform is the chemogenetic DREADD (designer receptor exclusively activated by designer drugs This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement cartilage-like matrix production, and it established hM3Dq as a powerful tool for elucidating the role of GPCR-mediated

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"Protecting neurons from death during oxidative and neuroexcitotoxic stress is key for preventing cognitive dysfunction. We uncovered a novel neuroprotective mechanism involving interaction between neurotrophic factor-α1 (NF-α1/carboxypeptidase E, CPE) and human 5-HTR1E, a G protein-coupled serotonin receptor with no previously known neurological function. Co-immunoprecipitation and pull-down assays confirmed interaction between NFα1/CPE and 5-HTR1E and 125I NF-α1/CPE-binding studies demonstrated saturable, high-affinity binding to 5-HTR1E in stably transfected HEK293 cells (Kd = 13.82 nM). Treatment of 5-HTR1E stable cells with NF-α1/CPE increased pERK 1/2 and pCREB levels which prevented a decrease in pro-survival protein, BCL2, during H2O2-induced oxidative stress. Cell survival assay in β-arrestin Knockout HEK293 cells showed that the NF-α1/CPE-5-HTR1E-mediated protection against oxidative stress was β-arrestin-dependent. Molecular dynamics studies revealed that NF-α1/CPE interacts with 5-HTR1E via 3 salt bridges, stabilized by several hydrogen bonds, independent of the serotonin pocket. Furthermore, after phosphorylating the C-terminal tail and intracellular loop 3 (ICL3) of NF-α1/CPE-5-HTR1E, it recruited β-arrestin1 by forming numerous salt bridges and hydrogen bonds to ICL2 and ICL3, leading to activation of β-arrestin1. Immunofluorescence studies showed 5-HTR1E and NF-α1/CPE are highly expressed and co-localized on cell surface of human hippocampal neurons. Importantly, knock-down of 5-HTR1E in human primary neurons diminished the NF-α1/CPE-mediated protection of these neurons against oxidative stress and glutamate neurotoxicity-induced cell death. Thus, NF-α1/CPE uniquely interacts with serotonin receptor 5-HTR1E to activate the β-arrestin/ERK/CREB/BCL2 pathway to mediate stress-induced neuroprotection." Read full article

partnerships and collaborations across pharma and #biotech⁠ and is an advocate for the role of #AI in drug Read more at the source #DrGPCR #GPCR #IndustryNews

Founded as a spinout from the University of Dundee on 20 July 2012, Exscientia pioneered the design of We have achieved a great deal in the last decade, such as the first-ever AI-designed drug candidates We’re excited about delivering the next ten years of Exscientia and advancing AI to design better drugs #artificialintelligence #drugdesign #drugdiscovery" Read more at the source #DrGPCR #GPCR #IndustryNews

chemistry decisions Why Live-cell High-Content Screening Matters for CB2 Ligand Profiling CB2 is a GPCR What This Means for CB2 Drug Discovery Programs Taken together, the dataset offers several insights into For researchers working in cannabinoid pharmacology, inflammation, or GPCR-mediated analgesia, these understandings of CB2 signaling, tools that preserve cellular context will be increasingly important for designing Three-dimensional quantitative structure–selectivity relationships analysis guided rational design of

In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while In this way, we present the analysis of a series of GPCRs whose activity has been shown to affect the Our compilation of data revealed that the mechanisms most involved in the role of GPCRs in lifespan are We also discuss the possibility of using agonist or antagonist drugs, depending on the beneficial or harmful effects of each GPCR, in order to prolong people's lifespan and healthspan.

protein-coupled receptor expression: Implications for metabolic regulation G protein-coupled receptors (GPCRs their secretion of insulin, and islet function can be modified by ligands acting at the large number of GPCRs is altered under pathophysiological conditions and, in this review, we have compared expression of GPCR We have also considered the likely outcomes on islet function that the altered GPCR expression status confers and the possible impact that adipokines, secreted from expanded fat depots, could have at those GPCRs

Watch Episode 169 What if you could earn a PhD while supporting a family and working full time in drug So I designed my own PhD program,” Sokhom shared. navigating work, life, and scientific ambition, Sokhom Pin proves it’s possible to have it all, if you design it yourself. _________________ Keyword Cloud: GPCR training program , GPCR scientist network , GPCR drug discovery , G protein-coupled receptors , GPCR online course

Therefore, the identification of such modulators as drug candidates is highly desirable. Currently, attention was mainly paid to biased signaling modulators targeting G protein-coupled receptors (GPCRs The biased signaling modulation of non-GPCR receptors has yet to be exploited. Toll-like receptor 4 (TLR4) is one such non-GPCR receptor, which involves MyD88-dependent and TRIF-dependent fine-tune receptor conformation and signaling but also provide an opportunity to identify promising drug

a startup delivering tools for GPCR drug discovery. were based on curiosity, instinct, and a surprising love of cooking (yes, she even compares molecule design Majellaro Now, she leads a team of talented chemists at Celtarys, developing fluorescent ligands that help drug GPCR on the company page . _______________ Keyword Cloud:   GPCR scientist network , career development GPCR ecosystem , GPCR podcast

of the Inflammatory Cytokine IL-6 and Is Dependent on NF-κB Signaling G protein-coupled receptors (GPCRs Members of the Mas-related G protein coupled receptors (MRGPRs), a subfamily of GPCRs, are largely expressed expressed in mast cells, macrophages, and in cardiovascular tissue, linking them to pseudo-allergic drug mediator and supports the notion that IL-6 can be used as a marker for MRGPRD activation in an in vitro drug