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December 2021 OMass Therapeutics's founder, Carol Robinson, has been awarded the prestigious Louis-Jeantet #DrugDiscovery #MassSpec #Award #massspectrometry" Read more at the source #DrGPCR #GPCR #IndustryNews

stage pharmaceutical company focused on the discovery, development, and commercialization of novel therapeutics Read more at the source #DrGPCR #GPCR #IndustryNews

Sosei Heptares Enters Antibody Discovery Agreement with Twist Bioscience to Discover and Develop Novel Therapeutic Antibodies against GPCR Targets "Collaboration aims to combine Twist’s proprietary synthetic antibody high-quality synthetic DNA using its silicon platform, announced a strategic collaboration to discover therapeutic antibodies against G protein-coupled receptors (GPCR) identified by Sosei Heptares." Read more at the source #DrGPCR #GPCR #IndustryNews

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

Ottawa, Ontario, Canada, Nov. 30, 2021 -- Orion Biotechnology, a clinical stage company unlocking the therapeutic potential of G Protein-Coupled Receptors (GPCRs) with a novel drug modality, proven discovery platform OB-004 is a GPCR targeted protein analog of CCL2 that targets the CCR2 receptor. Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Phase 1 studies in Japan with JNJ-40411813 (ADX71149) "Geneva, Switzerland, November 15, 2021 – Addex Therapeutics potential global development of ADX71149 for the treatment of epilepsy. " 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

Read more at the source #DrGPCR #GPCR #IndustryNews

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To target hard-to-drug targets like G protein-coupled receptors (GPCRs), more libraries, including better 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

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

stage pharmaceutical company focused on the discovery, development, and commercialization of novel therapeutics 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

essential for pipeline efficiency: How fast a ligand binds (k₁) and how long it stays bound (k₂)  can alter therapeutic When does onset rate dictate therapeutic onset, and when does offset rate predict duration? 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

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Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Kenakin highlights that therapeutic efficacy depends on the period during which a drug is actively engaged teams navigating development bottlenecks scientific leaders seeking clear pharmacological guidance GPCR

GPCRs represent major drug targets, as indicated by the fact that about 40% of all drugs currently used in clinical practice mediate their therapeutic effects by acting on GPCRs. Like many other organs, various GPCRs play a role in regulating liver function. It is predicted that more than 50 GPCRs are expressed in the liver. However, our knowledge of how GPCRs regulate liver metabolism and fibrosis in the different cell types

That choice determines whether you risk over- or under-dosing, miss safety windows, or miss therapeutic Kenakin walks through this as a living system , showing how GPCRs exist in multiple conformations and More nuanced control, fewer off-target liabilities, and novel therapeutic windows. Correctly distinguishing these mechanisms helps refine therapeutic index calculations, prioritize safer GPCR members save  50%+  (check your Weekly News code).