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- Addex Expands Pipeline With Selective M4 Positive Allosteric Modulator Program For The Treatment ...
Read more at the source #DrGPCR #GPCR #IndustryNews
- Allosteric Binding Data Interpretation in Complex Receptor Systems
In addition, while the field of GPCR science continues to expand with amazing and sometimes mindboggling foundational concepts laid out in the Corner will always be crucial for anyone studying or trying to modulate GPCR
- Why “Displacement” Misleads You: Allosteric Binding Demystified
If your project involves GPCRs , functional selectivity , or non-traditional ligands , this session is Subscribe to The Kenakin Brief today ➤ #AllostericPharmacology #GPCR #BindingVsFunction #ReceptorPharmacology
- 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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- 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 world-leading StaR® (stabilized receptor) platform to generate novel antibody leads to disease-relevant GPCR Cambridge, UK, 16 December 2021 – Sosei Group Corporation (“the Company”; TSE: 4565), the world leader in GPCR-focused announced a strategic collaboration to discover therapeutic antibodies against G protein-coupled receptors (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- 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
Read more at the source #DrGPCR #GPCR #IndustryNews
- 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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- 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
- 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
- Newly launched antibody libraries put hard-to-drug targets within reach
To target hard-to-drug targets like G protein-coupled receptors (GPCRs), more libraries, including better Read more at the source #DrGPCR #GPCR #IndustryNews
- Drug Discovery Pharmacology Principles That Turn Assays Into Real Medicines
teams navigating development bottlenecks scientific leaders seeking clear pharmacological guidance GPCR
- Dr. Alexander S. Hauser receives the Bachem award for peptide science
November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews
- How Fast Does a Drug Work?
s Corner  ______ #DrugDiscovery #Pharmacology #DrugKinetics #PipelineEfficiency #PharmaInnovation #GPCR
- Dr. Thomas P. Sakmar receives an honorary doctorate from Karolinska Institute
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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- Crinetics Pharmaceuticals announced the formation of an independently operated new company...
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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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- 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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- Orthosteric vs. Allosteric Interactions: The Silent Decider of Safety and Success
Kenakin walks through this as a living system , showing how GPCRs exist in multiple conformations and 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).
