Phase 1 results and supportive preclinical package assist in the launch of Phase 2 clinical development Metabolic successful completion of the Phase 1 Clinical Trial for its INV-202 molecule that focuses on treating metabolic Read more at the source #DrGPCR #GPCR #IndustryNews

We also identified two Gs-coupled GPCRs that are endogenously expressed by SKM at relatively high levels (β2-adrenergic receptor and CRF2 receptor) and studied the acute metabolic effects of activating these The acute metabolic effects following agonist activation of β2-adrenergic and, potentially, CRF2 receptors The acute metabolic effects of UCN2 were not mediated by SKM Gs signaling.

drug efficacy analyses, and toxicity studies; technologies that stabilize G protein–coupled receptors (GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

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compounds for Charcot-Marie-Tooth type 1A neuropathy (CMT1A) and pain. " Read more at the source #DrGPCR #GPCR

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August 2022 "WELCOME 4GPCRnet meeting bringing together four of the biggest GPCR networks in Europe for Four of the biggest European networks on GPCR research (COST Actions Adher’n Rise and ERNEST plus DFG-funded Read more at the source #DrGPCR #GPCR #IndustryNews

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antagonist of the arginine-vasopressin V2 receptor (V2R) and the only unique Kunitz-type peptide active on a GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Abstract Sigma receptor is a transmembrane non-GPCR protein expressed mainly in the endoplasmic Read more at the source #DrGPCR #GPCR #IndustryNews

"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

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position as Scientific co-founder LASEREDD Therapeutics" Ross Bathgate Read more at the source #DrGPCR #GPCR

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Tectonic Therapeutic, Inc. a pre-clinical stage biotechnology company transforming the discovery of novel GPCR-targeted Read more at the source #DrGPCR #GPCR #IndustryNews

issuance and will expire five years from their date of issuance. " Read more at the source #DrGPCR #GPCR

Corporation (“the Company”; TSE: 4565), an international biopharmaceutical company and world-leader in GPCR1 Read more at the source #DrGPCR #GPCR #IndustryNews

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discovery and development company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs Vice-President Drug Discovery, will present Orion’s novel technology for targeting undrugged peptidergic GPCRs discovery platform, one of the fastest drug discovery solutions in the industry for targeting peptidergic GPCRs antagonist, OB-004, demonstrating the ability of this powerful platform to rapidly identify best-in-class GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

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Translational Sciences Associate Director at Sosei Heptares, recently presented at the Keystone Symposia GPCR Read more at the source #DrGPCR #GPCR #IndustryNews