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584 items found for "GPCR therapeutics"
- Dr. Alexander S. Hauser receives the Bachem award for peptide science
November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews
- Dr. Thomas P. Sakmar receives an honorary doctorate from Karolinska Institute
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- Crinetics Pharmaceuticals announced the formation of an independently operated new company...
stage pharmaceutical company focused on the discovery, development, and commercialization of novel therapeutics Read more at the source #DrGPCR #GPCR #IndustryNews
- Perkins’ Head of Molecular Endocrinology and Pharmacology, Professor Kevin Pfleger, was appointed...
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- First in Human: Early-stage COVID therapies hold promise against omicron variant
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- Trevena Adds Seasoned Biopharma Commercial Executive to Senior Leadership Team
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- Search for safer pain relief advances with new engineered compounds
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- California gold rush for Sosei Heptares
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- Dr. Kevin Pfleger and Dr. Elizabeth Johnstone were awarded one of the 2022 Diabetes Research...
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- Positive Recommendation for Use of TAVNEOS™ (avacopan) in ANCA Vasculitis Adopted by European ...
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- Novel interaction between neurotrophic factor-α1/carboxypeptidase E and serotonin receptor, 5-HTR1E,
"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
- Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic ...
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
- Neurocrine Biosciences Presents Data on Treatment of Adolescent Patients with Classic Congenital ...
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- Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for ...
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
- InterAx Biotech AG and Boehringer Ingelheim take collaborate to unlock orphan targets leveraging ...
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
- G protein-coupled receptors that influence lifespan of human and animal models
In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while substantial participation in a wide variety of processes of human pathophysiology and are one of the main therapeutic 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
- Exscientia welcomes Richard J. Law, as their new Chief Business Officer
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- G protein-coupled receptor interactions and modification of signalling involving the ghrelin ...
GHSR1a The growth hormone secretagogue receptor 1a (GHSR1a) is intriguing because of its potential as a therapeutic Initial studies of the receptor focused on the potential therapeutic ability for growth hormone (GH) 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.
- Exscientia is 10 years old this July!
#artificialintelligence #drugdesign #drugdiscovery" Read more at the source #DrGPCR #GPCR #IndustryNews
- Functional molecular switches of mammalian G protein-coupled bitter-taste receptors
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
- Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas ...
Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas: a systematic and review Odorant receptors (ORs) account for about 60% of all human G protein-coupled receptors (GPCRs Glioma is the most common adult malignant brain tumor and requires novel therapeutic strategies to improve genomic and transcriptomic profiles of ORs in glioma, we suggest that ORs are potential biomarkers and therapeutic
- Recurrent high-impact mutations at cognate structural positions in class A G protein-coupled ...
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 and potential approaches to therapeutics.
- AcroScreen co-founder Margaux Duchamp has been selected as a 30 under 30 Europe Forbes ranking 2022
#ForbesUnder30 #ArcoScreen #sciences #EPFL" Read more at the source #DrGPCR #GPCR #IndustryNews
- Latrophilin-1 drives neuron morphogenesis and shapes chemo- and mechanosensation-dependent ...
mechanosensation-dependent behavior in C. elegans via a trans function Latrophilins are highly conserved Adhesion GPCRs
- In vivo metabolic effects after acute activation of skeletal muscle G s signaling
We also identified two Gs-coupled GPCRs that are endogenously expressed by SKM at relatively high levels
- Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled ..
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
- Profiling Immune Cell and Platelet Transcriptomes
processes and serving as critical targets for therapeutic interventions. ' roles in immune function and potential therapeutic applications. abundant and rare GPCR transcripts. could be targeted to modulate inflammatory responses, offering potential therapeutic avenues for conditions the field continues to evolve, the insights gained from this research will be instrumental in shaping therapeutic
- G.CLIPS biotech is 2 years old this month!
forward for more 🎊 #team #grateful #biotech #work #birthdaycelebration" Read more at the source #DrGPCR #GPCR