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September 2022 Divergent roles for the gut intraepithelial lymphocyte GLP-1R in control of metabolism , microbiota, and T cell-induced inflammation "Gut intraepithelial lymphocytes (IELs) are thought to proximal T cell receptor signaling in a protein-kinase-A-dependent manner. activation in gut IELs to modulation of microbiota composition and control of intestinal and systemic Read more at the source #DrGPCR #GPCR #IndustryNews

on the plasma membrane. Results obtained with the MRAP2 mutants R125H and R125C, which are found in human patients with extreme obesity, and mouse MRAP2, in which arginine 125 is normally replaced by histidine, were compared with those obtained with human MRAP2. of the MRAP2-PKR2 complex."

within myotubes and tissues of skeletal muscle from both murines and humans, thus representing a potentially Murine L6 skeletal muscle cells were used in order to clarify additional possible molecular signaling In conclusion, in skeletal muscle, CB1 receptors were recognized to be important moderators of NR4A1 and NR4A3 mRNA gene expression; these actions may have possible clinical benefits. Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 Ono Enters into Collaboration Agreement with Domain Therapeutics and Université de Montréal (Strasbourg, France; CEO: Pascal Neuville; “Domain”) and Université de Montréal (Québec, Canada; “UdM ”), to discover novel small molecules targeting G-Protein Coupled Receptors (GPCRs) in a metabolic disease Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "GPCRs in Medicinal Chemistry Event 8th RSC / SCI symposium on GPCRs in Medicinal Chemistry Dates Wednesday-Friday, 5th-7th October 2022 Place Evotec Campus Levi-Montalcini, Verona, Italy Downloads (bank transfers): Tuesday, 6th September 30th September – online registration (card payments)" Read more

are proud to announce that SYnAbs is now officially accredited as a Research Tax Credit by the French Ministry like to take this opportunity to thank all our French partners who trust us in the generation of their monoclonal antibodies against small molecules and transmembrane receptors! #technology #lifescience #immunology #antibodies #medicine #cancer #innovation #gpcr #synabs #monoclonalantibodies biologics #biotech #pharma #pharmaindustry #pharmaceuticals #oncology #healthcare #drugdevelopment" Read more

August 2022 "Abstract Rodent models are commonly used to evaluate parathyroid hormone (PTH) and PTH-related ion metabolism. Divergence, however, in the amino acid sequences of rodent and human PTH receptors (rat and mouse PTH1Rs PTH1R gene so that the human and not the mouse PTH1R protein is expressed. Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 Confo Therapeutics receives €1.7 million VLAIO grant for further research on GPCR modulators Therapeutics, founded in 2015 as a spin-off from VIB and VUB, announced today that it has been awarded a €1.7 million help expand Confo Therapeutic’s research on G protein-coupled receptor (GPCR) drug candidates. " Read more

June 2022 "Published on juin 22, 2022 On June 22, 2022, Michel Bouvier, Chief Executive Officer of IRIC , Principal Investigator of the Molecular Pharmacology Research Unit and Professor in the Department of Biochemistry and Molecular Medicine of the Faculty of Medicine of the Université de Montréal, is appointed Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR Binders, Drugs, and more In-depth molecular profiling of an intronic GNAO1 mutant as the basis for GPCRs in Cardiology, Endocrinology, and Taste Molecular Mechanisms of PTH/PTHrP Class B GPCR Signaling M Rosenkilde received two proof of concept grants from European Research Council (ERC) Addex Reports (May 22 - 26, 2023) 2nd LEAPS Meets Life Sciences Conference. (May 14 - 19, 2023) PEGS Boston (May 15 - 19, 2023) 8th and final ERNEST Meeting in Crete.

receptor (MOR) [1,6,7]. Molina, T.C. Südhof, and R.C. Malenka. 2013. K ´ onigstorfer, M. Mozhayeva, Y. Sara, T.C. Südhof, and ¨ E.T. Kavalali. 2001. Ma. 2008. Mol. Biol. 15:658–664.

summary of work performed both at Sosei Heptares and Glasgow University characterizing the role of the muscarinic M1 receptor in cognitive and neurodegenerative disorders and the potential therapeutic benefit of muscarinic M1 selective ligands." Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 Applying Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders This emerging class of small molecule drugs known as allosteric modulators is being explored for treating Addex did not invent allosteric modulation but is pioneering the screening technologies to find these difficult to locate molecules." Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 Addex Expands Pipeline With Selective M4 Positive Allosteric Modulator Program For The Treatment Psychotic Disorders "New Series of Potent and Selective Compounds Identified Using Proprietary Allosteric Modulator drug discovery and development, announced today that it has moved a selective and potent M4 muscarinic receptor positive allosteric modulator (PAM) program into lead optimization. Read more at the source #DrGPCR #GPCR #IndustryNews

March 2022 Inversago Pharma Announces Dosing of First Participant with Metabolic Syndrome in Phase 1B Clinical Trial "MONTREAL (CANADA) – March 15, 2022 – Inversago Pharma Inc. This 28-day trial will test the pharmacokinetics and safety profile of Inversago’s lead molecule, INV -202, on a targeted population with metabolic syndrome. Read more at the source #DrGPCR #GPCR #IndustryNews

effectors, activate downstream pathways that often modulate hallmark mechanisms of cancer. Because there are many more GPCRs than effectors, mutations in different receptors could perturb signaling We hypothesized that somatic mutations in tumor samples may not be enriched within a single gene but rather that cognate mutations with similar effects on GPCR function are distributed across many receptors of known functional motifs.

Electron cryo-microscopy (cryo-EM) is a powerful technique for the structural characterization of biological macromolecules, enabling high-resolution analysis of targets once inaccessible to structural interrogation Structural analysis of integral membrane proteins, which comprise a large proportion of druggable targets biologics, such as vaccines, viral vectors, and gene therapy agents, has also become significantly more As a result, cryo-EM has begun to make major impacts in bringing critical therapeutics to market.

Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled Receptor Members of the Mas-related G protein coupled receptors (MRGPRs), a subfamily of GPCRs, are largely expressed Several members of MRGPRs are also expressed in mast cells, macrophages, and in cardiovascular tissue (FBS) in the culture medium. as an inflammatory mediator and supports the notion that IL-6 can be used as a marker for MRGPRD activation

Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage Motoneuron (MN) IME by modulating background K+ channels TASK1. of MN IME via TASK1. TASK subunit in MNs), and primary cultures of embryonic spinal cord MNs (SMNs). MN IME was also augmented by the physiological neuromodulator lysophosphatidic acid (LPA) through a mechanism

this study was to determine the glucometabolic effects of acute activation of Gs signaling in skeletal muscle Methods: To address this question, we studied mice that express a Gs-coupled designer G protein-coupled receptor (Gs-DREADD or GsD) selectively in skeletal muscle. appear primarily mediated by altered insulin release. The acute metabolic effects of UCN2 were not mediated by SKM Gs signaling.

Latrophilin-1 drives neuron morphogenesis and shapes chemo- and mechanosensation-dependent behavior in via a trans function Latrophilins are highly conserved Adhesion GPCRs playing essential roles in the mammalian Recently, it has been shown that murine Latrophilins mediate classical G-protein signals to drive synaptogenesis Here, we show that Latrophilin-1 acts in trans to mediate morphogenesis of sensory structures in the analyses revealed specific LAT-1-positive neurons and first insights into the genetic network that is modulated

HDX-MS-optimized approach to characterize nanobodies as tools for biochemical and structural studies of class IB phosphoinositide 3-kinases There is considerable interest in developing antibodies as modulators ) pathway, which plays fundamental roles in growth, metabolism, and immunity. Ras and G protein-coupled receptors (GPCRs) to mediate its cellular roles. nanobodies using hydrogen-deuterium exchange (HDX) mass spectrometry (MS) for structural and biochemical

The mammalian target of rapamycin (mTOR) senses upstream stimuli to regulate numerous cellular functions such as metabolism, growth, and autophagy. The activation of mTOR complex 1 (mTORC1) is typically observed in human disease and continues to be Understanding the upstream regulators of mTORC1 will provide a crucial link to targeting mTORC1 hyperactivated Significance Statement mTORC1 is a master regulator of many cellular processes and is often hyperactivated

Mutations in G protein-coupled receptors (GPCRs) underlie numerous diseases. Many cause receptor misfolding and failure to reach the cell surface. Pharmacological chaperones are cell-permeant small molecules that engage nascent mutant GPCRs in the We previously demonstrated rescue of cell surface expression of luteinizing hormone receptor mutants receptors (FSHRs) with poor cell surface expression using a small-molecule FSHR agonist, CAN1404.

Currently, attention was mainly paid to biased signaling modulators targeting G protein-coupled receptors of biased modulator development targeting TLR4. The challenges and methods for the discovery of TLR4 biased modulators are also outlined. Small molecules biasedly modulating the TLR4 signaling axis not only provide probes to fine-tune receptor modulators for other non-GPCR receptors.

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High-affinity agonists reveal recognition motifs for the MRGPRD GPCR Chunyu Wang ,  Yongfeng Liu ,  Marion ,  Dominic R Huxley ,   Peter Gmeiner ,  Peter J McCormick ,  Dorothee Weikert ,  Masha Y Niv ,  Moran Schedule a session with our Chief Match Maker. Direct line to the Dr. GPCR community members Connect with fellow GPCR enthusiasts :) So much more to come! Major Announcement!