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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

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

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control neuropsychiatric symptoms in conditions such as schizophrenia. " Read more at the source #DrGPCR #GPCR

These molecules are then evaluated at unprecedented speed and scale on hundreds of GPCR targets simultaneously Read more at the source #DrGPCR #GPCR #IndustryNews

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Changes to Drive the Company Through the Next Stage of its Evolution "New team focused on expanding its GPCR-focused Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 Read more at the source #DrGPCR #GPCR #IndustryNews

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If your project involves GPCRs , functional selectivity , or non-traditional ligands , this session is Subscribe to The Kenakin Brief today ➤ #AllostericPharmacology #GPCR #BindingVsFunction #ReceptorPharmacology

– Confo Therapeutics, a leader in the discovery of medicines targeting G-protein coupled receptors (GPCRs pharmacokinetics of CFTX-1554 in healthy subjects (NCT05260658). " Read more at the source #DrGPCR #GPCR

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February 2022 Read more at the source #DrGPCR #GPCR #IndustryNews

Collaborative efforts aim to accelerate and improve the prediction of first-in-class small molecule agonists for a challenging orphan GPCR for a highly relevant therapeutic need. 💊 InterAx Biotech AG discovery successfully applied in projects with biopharmaceutical companies and also used in-house to discover first-in-class #ai #biotech #systemsbiology #drugdiscovery #gpcr #deeptech #orphandrugs #pharma #partnerships #AI4drugdiscovery " Read more at the source #DrGPCR #GPCR #IndustryNews

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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 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 leaders who need credible guidance fast, the Corner brings clarity to the complexities shaping modern GPCR

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December 2021 "30/11/2021 Confo will work together with Regeneron to apply its GPCR drug discovery platform technology platform, which uses conformationally selective VHH antibodies – ConfoBodies® – to stabilize GPCRs enabling the discovery of novel therapeutic antibody drug candidates. " Read more at the source #DrGPCR #GPCR

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Discovery Agreement with Twist Bioscience to Discover and Develop Novel Therapeutic Antibodies against GPCR world-leading StaR® (stabilized receptor) platform to generate novel antibody leads to disease-relevant GPCR Cambridge, UK, 16 December 2021 – Sosei Group Corporation (“the Company”; TSE: 4565), the world leader in GPCR-focused announced a strategic collaboration to discover therapeutic antibodies against G protein-coupled receptors (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

The targets, including G protein-coupled receptors (GPCRs), intracellular protein complexes and solute Read more at the source #DrGPCR #GPCR #IndustryNews