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- Applying Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders with ...
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- Crinetics Pharmaceuticals Announces Pricing Of Underwritten Common Stock Offering
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- Addex Therapeutics Completes Patient Enrollment For Dipraglurant Blepharospasm Phase 2 Clinical ...
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- Sosei Heptares Enters Antibody Discovery Agreement with Twist Bioscience to Discover and Develop ...
Discovery Agreement with Twist Bioscience to Discover and Develop Novel Therapeutic Antibodies against GPCR Targets "Collaboration aims to combine Twist’s proprietary synthetic antibody libraries and sophisticated world-leading StaR® (stabilized receptor) platform to generate novel antibody leads to disease-relevant GPCR announced a strategic collaboration to discover therapeutic antibodies against G protein-coupled receptors (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Addex Expands Pipeline With Selective M4 Positive Allosteric Modulator Program For The Treatment ...
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- Sosei Heptares reported its FY2021 financial result and provided an update on operational activities
February 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 Complex Two-Stage Biology Behind Orthosteric Binding GPCR pharmacology rarely follows the neat Langmuir Through deep-dive lectures, monthly AMAs, and a growing on-demand library, the Corner helps discovery Corner and the broader Ecosystem Premium. 40 years of expertise at your fingertips : Explore the full library
- 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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- Orion Announces The Rapid Lead Optimization Of Ob-004 - A Ccr2 Antagonist
Biotechnology, a clinical stage company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs OB-004 is a GPCR targeted protein analog of CCL2 that targets the CCR2 receptor. Read more at the source #DrGPCR #GPCR #IndustryNews
- VIB spin-off Confo Therapeutics Enters Collaborative Agreement with Regeneron
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
- ShouTi Pharma has a brand new website
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- Learn more about Neurocrine Biosciences with their new video
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- Trevena Announce Submission of New Drug Application in China for OLINVYK® by its Partner Jiangsu ...
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- Finding needles in haystacks: Omass unveils pipeline aimed at tough-to-drug targets
The targets, including G protein-coupled receptors (GPCRs), intracellular protein complexes and solute Read more at the source #DrGPCR #GPCR #IndustryNews
- Why “Displacement” Misleads You: Allosteric Binding Demystified
If your project involves GPCRs , functional selectivity , or non-traditional ligands , this session is Terry Kenakin An always-growing library of on-demand pharmacology insights The ability to vote on or Don’t just keep up, get ahead. 🟢 40 years of expertise at your fingertips: Explore the complete library Subscribe to The Kenakin Brief today ➤ #AllostericPharmacology #GPCR #BindingVsFunction #ReceptorPharmacology
- 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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- Search for safer pain relief advances with new engineered compounds
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- Crinetics Pharmaceuticals announced the formation of an independently operated new company...
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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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- Addex's strategic partner The Janssen Pharmaceutical Companies of Johnson & Johnson, Inc. has...
potential global development of ADX71149 for the treatment of epilepsy. " Read more at the source #DrGPCR #GPCR
- Neurocrine Biosciences Presents Data on Treatment of Adolescent Patients with Classic Congenital ...
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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
- How Fast Does a Drug Work?
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