Read more at the source #DrGPCR #GPCR #IndustryNews

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

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

If your project involves GPCRs , functional selectivity , or non-traditional ligands , this session is Subscribe to The Kenakin Brief today ➤ #AllostericPharmacology #GPCR #BindingVsFunction #ReceptorPharmacology

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

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

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

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

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

"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

In reality, it represents something very different: EC₅₀ is a system-dependent measure of functional A ligand may show identical EC₅₀ values in two assays while engaging receptors through very different Two compounds with identical potency may behave very differently in vivo if one remains bound longer. teams navigating development bottlenecks scientific leaders seeking clear pharmacological guidance GPCR

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

s Corner   ______ #DrugDiscovery #Pharmacology #DrugKinetics #PipelineEfficiency #PharmaInnovation #GPCR

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

Kenakin walks through this as a living system , showing how GPCRs exist in multiple conformations and That perspective helps explain why two compounds with similar affinities can deliver very different clinical cleaner assay design but a sharper decision framework for selecting, prioritizing, and dosing your lead series 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).

Read more at the source #DrGPCR #GPCR #IndustryNews

Prof Pfleger has served on the ASCEPT Board since 2016 and was Chair of the Scientific Advisory Committee Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

This dataset highlights how HCS can be used both to triage compound series and to extract quantitative chemistry decisions Why Live-cell High-Content Screening Matters for CB2 Ligand Profiling CB2 is a GPCR For GPCR programs—where trafficking, receptor reserve, and internalization are common confounders—access to these images supports more confident cross-series comparisons. For researchers working in cannabinoid pharmacology, inflammation, or GPCR-mediated analgesia, these

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews