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

Dr. s Corner   ______ #DrugDiscovery #Pharmacology #DrugKinetics #PipelineEfficiency #PharmaInnovation #GPCR

To target hard-to-drug targets like G protein-coupled receptors (GPCRs), more libraries, including better Read more at the source #DrGPCR #GPCR #IndustryNews

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Dr. Kenakin walks through this as a living system , showing how GPCRs exist in multiple conformations and stay ahead of the science 🧠 Content built for biotech, pharma & academia 💬 Live monthly AMA with Dr Kenakin     💎 $2999/year — one conference cost = 12 months of expert training  Premium Dr. GPCR members save  50%+  (check your Weekly News code).

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potential global development of ADX71149 for the treatment of epilepsy. " Read more at the source #DrGPCR #GPCR

"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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In the full lecture, Dr. Linearity  of the Schild regression (log(DR–1) vs. antagonist concentration). As Dr. Watch the course trailer 👇 Why Terry’s Corner Weekly pharmacology lectures by Dr. GPCR innovation is accelerating—those who act now will define tomorrow’s breakthroughs.

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. However, our knowledge of how GPCRs regulate liver metabolism and fibrosis in the different cell types

accelerate and improve the prediction of first-in-class small molecule agonists for a challenging orphan GPCR #ai #biotech #systemsbiology #drugdiscovery #gpcr #deeptech #orphandrugs #pharma #partnerships #AI4drugdiscovery " Read more at the source #DrGPCR #GPCR #IndustryNews

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

chemistry decisions Why Live-cell High-Content Screening Matters for CB2 Ligand Profiling CB2 is a GPCR For GPCR programs—where trafficking, receptor reserve, and internalization are common confounders—access For researchers working in cannabinoid pharmacology, inflammation, or GPCR-mediated analgesia, these

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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 possibility of using agonist or antagonist drugs, depending on the beneficial or harmful effects of each GPCR

#artificialintelligence #drugdesign #drugdiscovery" Read more at the source #DrGPCR #GPCR #IndustryNews

Plus, check out the latest Dr. GPCR tools and key moves in the biotech world. Dr. Become a Dr. GPCR Ambassador - Share & refer with Dr. GPCR.   Help grow the GPCR community by joining the Dr. GPCR affiliate program. GPCR University - A fast-reference guide for you!   The Dr. Best wishes, The Dr. GPCR Team

vitro and in vivo data suggest that GHSR1a heterodimerises with multiple G protein-coupled receptors (GPCRs This review discusses the signalling mechanisms of GHSR1a alone and in combination with other GPCRs, and explores the physiological consequences of GHSR1a coupling with other GPCRs.

GPCR Colleagues & Curiosity-Driven Minds, We’re starting with exciting Dr. with Dr. Dr. Access the Course Dr. GPCR Symposia  – On-demand talks from GPCR trailblazers   Watch anytime. Stay curious, The Dr. GPCR Team

Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs Using current knowledge on class A GPCRs and existing experimental data in the literature as constraints

#ForbesUnder30 #ArcoScreen #sciences #EPFL" Read more at the source #DrGPCR #GPCR #IndustryNews

Hello GPCR Innovators ,   We’re preparing to launch Terry’s Corner, a new knowledge hub shaped by Dr. Terry Kenakin’s decades of GPCR insight. Plus, Celtarys explores ligand selection for better assays, and co-founder Dr. Screens with Dr. Best,   The Dr. GPCR Team