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Results found for "GPCR Drug Design"
- Michel Bouvier appointed Knight of the Ordre national du Québec
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- Crinetics Presents Clinical And Research Results At ENDO 2022
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- ShouTi Pharma CEO Dr. Raymond Stevens was interviewed by Moira Gunn of the NPR TechNation podcast
April 2022 Read more at the source #DrGPCR #GPCR #IndustryNews
- Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls
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 Proper orthosteric binding design prevents those errors before they propagate into SAR narratives. 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
- Search for safer pain relief advances with new engineered compounds
in Florida have created a collection of new pain-relieving compounds that, like morphine and other drugs Read more at the source #DrGPCR #GPCR #IndustryNews
- John Streicher talks about his work on terpenes found in cannabis as these may be a novel way to ...
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- Modulation of Striatal Adenosinergic Function by HTL0041178, a Selective GPR52 Agonist
control neuropsychiatric symptoms in conditions such as schizophrenia. " Read more at the source #DrGPCR #GPCR
- Trevena Receives up to $40M in OLINVYK ex-US Royalty-Based Financing from R-Bridge Healthcare ...
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- Inversago Pharma appoints Glenn S. Vraniak as Chief Financial Officer
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- Trevena Announces Receipt of First $15 million Tranche in Connection with its $40 million ...
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- Crinetics Pharmaceuticals announced the formation of an independently operated new company...
Provided by 5AM and Frazier – Pipeline is Built from Crinetics’ Core Nonpeptide Platform and Includes Drug Read more at the source #DrGPCR #GPCR #IndustryNews
- Crinetics Pharmaceuticals Announces Pricing Of Underwritten Common Stock Offering
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- Addex's strategic partner The Janssen Pharmaceutical Companies of Johnson & Johnson, Inc. has...
ADXN and Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based drug potential global development of ADX71149 for the treatment of epilepsy. " Read more at the source #DrGPCR #GPCR
- Sosei Heptares reported its FY2021 financial result and provided an update on operational activities
February 2022 Read more at the source #DrGPCR #GPCR #IndustryNews
- Crinetics Pharmaceuticals Expands Executive Team With Appointment Of James Hassard As Chief ...
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- Inversago Pharma Announces Dosing of First Participant with Metabolic Syndrome in Phase 1B ...
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- 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. cells that regulate liver fibrosis, may lead to the development of drugs that can improve hepatic fibrosis
- ShouTi Pharma has a brand new website
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- Learn more about Neurocrine Biosciences with their new video
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- 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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- 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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- 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
- Targeted Activation of G-Protein Coupled Receptor-Mediated Ca 2+ Signaling Drives Enhanced Cartilage
One such platform is the chemogenetic DREADD (designer receptor exclusively activated by designer drugs This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement cartilage-like matrix production, and it established hM3Dq as a powerful tool for elucidating the role of GPCR-mediated
- Neurocrine Biosciences Presents Data on Treatment of Adolescent Patients with Classic Congenital ...
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