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

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

– Confo Therapeutics, a leader in the discovery of medicines targeting G-protein coupled receptors (GPCRs treatment of neuropathic pain, a debilitating condition caused by damage to the nerves outside of the brain pharmacokinetics of CFTX-1554 in healthy subjects (NCT05260658). " Read more at the source #DrGPCR #GPCR

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But here’s the truth: too many programs still fail because early decisions were built on shaky mechanistic Equip your team with this literacy now to design cleaner pharmacology and accelerate smarter, safer programs Watch our new trailers for a preview of expert-led GPCR training designed for scientists and drug hunters Kenakin     💎 $2999/year — one conference cost = 12 months of expert training  Premium Dr. GPCR members save  50%+  (check your Weekly News code).

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

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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

Drug discovery programs rarely fail because an assay produced poor data. EC₅₀ Misconceptions Persist Few misunderstandings derail discovery programs faster than misinterpreting When PK Ends Programs Discovery teams often fall in love with molecules that show beautiful activity Failure Is the Real Curriculum Drug discovery carries a difficult truth: most programs fail. teams navigating development bottlenecks scientific leaders seeking clear pharmacological guidance GPCR

Kenakin’s kinetic insights help you translate assay readouts into actionable knowledge that keeps your programs Don’t Let Outdated Models Slow Your Next Program The analytical tools that shaped traditional affinity s Corner   ______ #DrugDiscovery #Pharmacology #DrugKinetics #PipelineEfficiency #PharmaInnovation #GPCR

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"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

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

chemistry decisions Why Live-cell High-Content Screening Matters for CB2 Ligand Profiling CB2 is a GPCR For cannabinoid chemistry programs—where small structural shifts can significantly alter receptor preference For GPCR programs—where trafficking, receptor reserve, and internalization are common confounders—access What This Means for CB2 Drug Discovery Programs Taken together, the dataset offers several insights into For researchers working in cannabinoid pharmacology, inflammation, or GPCR-mediated analgesia, these

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The omicron strain of the virus was first identified in South Africa in early November, and an existing Read more at the source #DrGPCR #GPCR #IndustryNews

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