April 2022 Read more at the source #DrGPCR #GPCR #IndustryNews

Series of Potent and Selective Compounds Identified Using Proprietary Allosteric Modulator Screening Platform Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

control neuropsychiatric symptoms in conditions such as schizophrenia. " Read more at the source #DrGPCR #GPCR

Read more at the source #DrGPCR #GPCR #IndustryNews

– Confo Therapeutics, a leader in the discovery of medicines targeting G-protein coupled receptors (GPCRs pharmacokinetics of CFTX-1554 in healthy subjects (NCT05260658). " Read more at the source #DrGPCR #GPCR

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

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

Application in China for OLINVYK® by its Partner Jiangsu Nhwa Pharmaceutical "Submission supported by data Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Discovery Agreement with Twist Bioscience to Discover and Develop Novel Therapeutic Antibodies against GPCR sophisticated bioinformatics expertise with Sosei Heptares’ world-leading StaR® (stabilized receptor) platform to generate novel antibody leads to disease-relevant GPCR targets Tokyo, Japan and Cambridge, UK, 16 enabling customers to succeed through its offering of high-quality synthetic DNA using its silicon platform Read more at the source #DrGPCR #GPCR #IndustryNews

February 2022 Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Biotechnology, a clinical stage company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs ) with a novel drug modality, proven discovery platform and best-in-class molecules, today announced OB-004 is a GPCR targeted protein analog of CCL2 that targets the CCR2 receptor. Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 "30/11/2021 Confo will work together with Regeneron to apply its GPCR drug discovery platform entered into a collaborative agreement with Regeneron Pharmaceuticals, Inc. whereby Confo’s technology platform , which uses conformationally selective VHH antibodies – ConfoBodies® – to stabilize GPCRs (G protein-coupled enabling the discovery of novel therapeutic antibody drug candidates. " Read more at the source #DrGPCR #GPCR

Read more at the source #DrGPCR #GPCR #IndustryNews

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).

"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

The targets, including G protein-coupled receptors (GPCRs), intracellular protein complexes and solute Read more at the source #DrGPCR #GPCR #IndustryNews

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.

To target hard-to-drug targets like G protein-coupled receptors (GPCRs), more libraries, including better Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews

in Initial Financing Provided by 5AM and Frazier – Pipeline is Built from Crinetics’ Core Nonpeptide Platform Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews