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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

chemistry decisions Why Live-cell High-Content Screening Matters for CB2 Ligand Profiling CB2 is a GPCR Providing full tracer information ensures that researchers can recalculate or align affinity values across platforms Physiological context strengthens data reliability.   profiling binding directly in intact HEK-293 cells, the assay reduces artefacts common in membrane-based platforms exploring biased agonism, polypharmacology, or downstream signaling—live-cell HCS provides a rigorous platform

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

take first steps towards collaborating to unlock orphan targets leveraging InterAx AI driven discovery platform 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 platform was already successfully #ai #biotech #systemsbiology #drugdiscovery #gpcr #deeptech #orphandrugs #pharma #partnerships #AI4drugdiscovery " Read more at the source #DrGPCR #GPCR #IndustryNews

Kenakin walks through this as a living system , showing how GPCRs exist in multiple conformations and One of the most powerful aspects of this session is how it reframes the questions you ask of your own data Watch our new trailers for a preview of expert-led GPCR training designed for scientists and drug hunters GPCR members save  50%+  (check your Weekly News code).

discovery often assumes receptor inhibition follows simple rules—agonist binds, antagonist blocks, and data receptor pharmacology into detective work, spotlighting mechanistic fingerprints buried in dose–response data Even when maximal responses are altered, affinity constants remain extractable  from correctly chosen data GPCR innovation is accelerating—those who act now will define tomorrow’s breakthroughs.

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

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

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In vitro and in vivo data suggest that GHSR1a heterodimerises with multiple G protein-coupled receptors (GPCRs), including dopamine D1 and D2, serotonin 2C, orexin, oxytocin and melanocortin 3 receptors ( 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.

first-ever AI-designed drug candidates to enter clinical trials, the first AI-driven precision medicine platform #artificialintelligence #drugdesign #drugdiscovery" Read more at the source #DrGPCR #GPCR #IndustryNews

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

structural positions in class A G protein-coupled receptors expressed in tumors G protein-coupled receptors (GPCRs Because there are many more GPCRs than effectors, mutations in different receptors could perturb signaling may not be enriched within a single gene but rather that cognate mutations with similar effects on GPCR To test this possibility, we systematically aggregated somatic cancer mutations across class A GPCRs These data suggest that recurrent impactful oncogenic mutations perturb different GPCRs to subvert signaling

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

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mechanosensation-dependent behavior in C. elegans via a trans function Latrophilins are highly conserved Adhesion GPCRs

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We also identified two Gs-coupled GPCRs that are endogenously expressed by SKM at relatively high levels

of the Inflammatory Cytokine IL-6 and Is Dependent on NF-κB Signaling G protein-coupled receptors (GPCRs Members of the Mas-related G protein coupled receptors (MRGPRs), a subfamily of GPCRs, are largely expressed MRGPRD) in the regulation of the inflammatory mediator interleukin 6 (IL-6) has not been demonstrated to date

receptor-ligand complexes: Impact of ligand type and receptor activation state G protein-coupled receptors (GPCR Their abundance and role in nearly all physiological systems make GPCR the largest protein family targeted provided broadly generalizable performance expectations for docking into experimentally-characterized GPCR Simulations were performed using 37 experimental structures of 11 Class A GPCR crystallized in multiple Therefore, docking performance against GPCR targets can be estimated in advance based on docking target

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Join Terry’s Corner Today Yamina’s Corner Is Live – Are you drowning in disorganized data? Because even the best data means nothing without structure. That’s the Lego Bucket Problem.    affinity, high specificity, and a strong signal-to-noise profile, this non-radioactive, cell-compatible platform Read The Full Article GPCR Publication Highlights   Chemokine–GPCR Selectivity Unveiled Sequence- and GPCR Team Join Our Newsletter!

Lysophosphatidic acids (LPAs) are bioactive phospholipids implicated in a wide range of cellular activities that regulate a diverse array of biological functions. They recognize two types of G protein-coupled receptors (LPARs): LPA1-3 receptors and LPA4-6 receptors that belong to the endothelial gene (EDG) family and non-endothelial gene family, respectively. In recent years, the LPA signaling pathway has captured an increasing amount of attention because of its involvement in various diseases, such as idiopathic pulmonary fibrosis, cancers, cardiovascular diseases and neuropathic pain, making it a promising target for drug development. While no drugs targeting LPARs have been approved by the FDA thus far, at least three antagonists have entered phase Ⅱ clinical trials for idiopathic pulmonary fibrosis (BMS-986020 and BMS-986278) and systemic sclerosis (SAR100842), and one radioligand (BMT-136088/18F-BMS-986327) has entered phase Ⅰ clinical trials for positron emission tomography (PET) imaging of idiopathic pulmonary fibrosis. This article provides an extensive review on the current status of ligand development targeting LPA receptors to modulate LPA signaling and their therapeutic potential in various diseases. Read full article

G protein-coupled receptors (GPCRs) are integral to cellular signaling, influencing a wide array of physiological A study published in Scientific Data by Arne Hansen et a l has introduced a sensitive method for detecting of GPCRs' roles in immune function and potential therapeutic applications. to 206, while platelets exhibit a distinct profile with 69 GPCR mRNAs. abundant and rare GPCR transcripts.

Ho, ho, ho, GPCR elves! As researchers, we all understand the importance of data in driving meaningful discoveries  and advancing GPCR ecosystem! Best, Yamina & the Dr. Classified GPCR News  Let’s dive into the   Classified GPCR News from December 9th to 15th, 2024 Industry and TPD Structural Biology Platforms GPCR Events, Meetings, and Webinars December 10 - 12, 2024 |

#technology #lifescience #immunology #antibodies #medicine #cancer #innovation #gpcr #synabs #monoclonalantibodies pharmaindustry #pharmaceuticals #oncology #healthcare #drugdevelopment" Read more at the source #DrGPCR #GPCR

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. delivers selective pain relief in preclinical models Dr.GPCR Updates Terry’s Corner  – Build Better GPCR Celtarys explores how fluorescent ligands enable safer, high-throughput screening with rich kinetic data GPCR Team

pharmaceutical chemist, Alessandro never imagined himself working at the cutting edge of computational GPCR began their mission: to computationally study olfactory GPCRs , a massively under-characterized group With hundreds of subtypes and limited ligand data, olfactory GPCRs represent a high-risk, high-reward —Alessandro Nicoli Want to explore computational GPCR science yourself? Explore the   GPCR University  or enroll in Terry's Corner for GPCR Courses led by Dr.