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powerful technique for the structural characterization of biological macromolecules, enabling high-resolution In recent years, pharmaceutical companies have begun to utilize cryo-EM for structure-based drug design As a result, cryo-EM has begun to make major impacts in bringing critical therapeutics to market. In this review, we discuss recent instructive examples of impacts from cryo-EM in therapeutics design Read full article

G-protein coupled receptors (GPCRs) play a paramount role in diverse brain functions. Almost 20 years ago, GPCR activity was shown to be regulated by membrane potential in vitro, but whether Depolarization alone, without a muscarinic agonist, results in a nicotinic ionotropic receptor potentiation that is mediated by muscarinic receptor voltage dependency. Read full article

Arrestins regulate a wide range of signaling events, most notably when bound to active G protein-coupled receptors (GPCRs). Among the known effectors recruited by GPCR-bound arrestins are Src family kinases, which regulate cellular , consistent with a role as a signaling scaffold. Read full article

Engineered G protein-coupled receptors (GPCRs) are commonly used in chemogenetics as designer receptors Although several GPCRs have been studied in astrocytes using a chemogenetic approach, the functional role of the astrocytic Gi pathway is not clear, as the literature is conflicting depending on the brain regions Taken together, our results indicate that the astrocytic Gi pathway plays an inhibitory role in neuroinflammation Read full article

G protein-coupled receptors (GPCRs) are among the most promising drug targets. They often form homo- and heterodimers with allosteric cross-talk between receptor entities, which contributes transmembrane domain, which also controls the constitutive activity of the GABAB receptor. of the receptors. Read full article

. elegans via a trans function Latrophilins are highly conserved Adhesion GPCRs playing essential roles This trans function is physiologically relevant in copulation behavior. Detailed expression and RNA-Seq analyses revealed specific LAT-1-positive neurons and first insights into the genetic network that is modulated by the receptor function. Read full article

pathways in higher eukaryotes is the phosphoinositide 3-kinase (PI3K) pathway, which plays fundamental roles and G protein-coupled receptors (GPCRs) to mediate its cellular roles. We identify nanobodies that stimulated lipid kinase activity, block Ras activation, and specifically Overall, our work reveals insight into PI3Kγ regulation and identifies sites that may be exploited for Read full article

Four of the biggest European networks on GPCR research ( COST Actions Adher’n Rise and ERNEST plus DFG-funded CRC1423 and RU2372 ) have joined forces to organize an international meeting, which will We aim to connect renowned international experts of the field with early career ‘rising stars’.

We are closely monitoring any regulation changes from both Boston and Massachusetts with regard to in-person Please refer to our Safe Meeting guidelines for information about how you can participate in the event Don't miss the chance to present your innovative research at this year's conference. Register here

programming packages for cheminformatics and structural bioinformatics are powerful tools to build modular, reproducible , and reusable pipelines for computer-aided drug design (CADD). both the theoretical as well as practical aspect of these topics, the platform addresses students and researchers an interactive Jupyter Notebook is offered, using open source packages such as the Python packages rdkit

Perth next year, in collaboration with the Australasian Pharmaceutical Science Association ( APSA ).” " Read

identified in South Africa in early November, and an existing treatment has already shown positive results While vaccine-makers race to test their shots against the variant, the monoclonal antibody sotrovimab from Vir and partner GlaxoSmithKline PLC posted results Dec. 7 demonstrating activity against the omicron Read more at the source #DrGPCR #GPCR #IndustryNews

libraries and sophisticated bioinformatics expertise with Sosei Heptares’ world-leading StaR® (stabilized receptor ) platform to generate novel antibody leads to disease-relevant GPCR targets Tokyo, Japan and Cambridge , announced a strategic collaboration to discover therapeutic antibodies against G protein-coupled receptors (GPCR) identified by Sosei Heptares . " Read more at the source #DrGPCR #GPCR #IndustryNews

Learn about his remarkable career and research in #GPCR signaling and trafficking.

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The targets, including G protein-coupled receptors (GPCRs), intracellular protein complexes and solute carriers, are relevant to immunology indications and rare diseases with high unmet need." Read more at the source #DrGPCR #GPCR #IndustryNews

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Sakmar on how the molecular studies of rhodopsin paved the way to understanding #GPCRs Be sure to subscribe

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