August 2022 A new Kunitz-type snake toxin family associated with an original mode of interaction with the vasopressin 2 receptor "Abstract Background and purpose: Venomous animals express numerous Kunitz-type peptides. The mambaquaretin-1 (MQ1) peptide identified from the Dendroaspis angusticeps venom is the most selective antagonist of the arginine-vasopressin V2 receptor (V2R) and the only unique Kunitz-type peptide active on a GPCR. We aimed to exploit other mamba venoms to enlarge the V2R-Kunitz peptide family and gain insight into the MQ1 molecular mode of action. Experimental approach: We used a bio-guided screening assay to identify novel MQs and placed them phylogenetically. MQs were produced by solid-phase peptide synthesis and characterized in vitro by binding and functional tests and in vivo by diuresis measurement in rats. Key results: Eight additional MQs were identified with nanomolar affinities for the V2R, all antagonists. MQs form a new subgroup in the Kunitz family, close to the V2R non-active dendrotoxins and to two V2R-active cobra toxins. Sequence comparison between active and non-active V2R Kunitz peptides highlighted five positions, among which four are involved in V2R interaction and belong to the two large MQ1 loops. We finally determined that eight positions, part of these two loops, interact with the V2R. The variant MQ1-K39A showed a higher affinity for the hV2R, but not for the rat V2R. Conclusions and implications: A new function and mode of action is associated with the Kunitz peptides. The number of MQ1 residues involved in V2R binding is large and may explain its absolute selectivity. MQ1-K39A represents the first step in the improvement of the MQ1 design from a medicinal perspective." Read more at the source #DrGPCR #GPCR #IndustryNews

Significant advancements in the cellular biology of G protein-coupled receptors (GPCRs) about a novel biosensor shed light on the endosomal proteome associated with the δ-opioid receptor (DOR). This study, published in Nature Chemical Biology, highlights the role of the chaperone protein DNAJC13 the endosomal proteome associated with the DOR receptor. labeled by APEX2) and analyzed them using quantitative proteomics such as tandem mass tags.

Through bioinformatic analysis of lysosomal proteomes, we identified lysosomal cholesterol signaling (LYCHOS, previously annotated as G protein-coupled receptor 155), a multidomain transmembrane protein that enables cholesterol-dependent activation of the master growth regulator, the protein kinase mechanistic concentrations, LYCHOS bound to the GATOR1 complex, a guanosine triphosphatase (GTPase)-activating protein

October 2022 "The very large G protein-coupled receptor (VLGR1, ADGRV1) is the largest member of the Affinity proteomics revealed that in the interactome of VLGR1, molecules are enriched that are associated We confirmed the interaction of VLGR1 with key proteins of MAMs by pull-down assays in vitro complemented

Research Middle-Down Mass Spectrometry Reveals Activity-Modifying Phosphorylation Barcode in a Class C G Protein-Coupled Current Technologies To Understand G-Protein-Coupled Receptor Molecular Pharmacology. The Illuminating the Understudied Druggable Proteome Conference.

FSLLRY-NH2, a protease-activated receptor 2 (PAR2) antagonist, activates mas-related G protein-coupled ACE2 Activation by Tripeptide IRW (Ile-Arg-Trp) Depends on the G Protein-Coupled Receptor 30 Signaling The Illuminating the Understudied Druggable Proteome Conference.

GPCRs in Oncology and Immunology Pan-cancer functional analysis of somatic mutations in G protein-coupled Updates in GPCR Research 3,4-Bis(hydroxymethyl)hexane-1,6-diol-based Maltosides (HDMs) for Membrane-Protein Study: Importance of Detergent Rigidity-Flexibility Balance in Protein Stability. iORbase: a database Deadline February 12, 2023 Current Technologies To Understand G-Protein-Coupled Receptor Molecular Pharmacology The Illuminating the Understudied Druggable Proteome Conference.

Regulation of the pro-inflammatory G protein-coupled receptor GPR84. GPCRs in Neuroscience G protein coupled receptors as targets for transformative neuropsychiatric therapeutics The Illuminating the Understudied Druggable Proteome Conference. Research - Senior Scientist, Cell-Based Assay Development Post Doctoral Fellow Research associate in protein

Deadline February 12, 2023 Current Technologies To Understand G-Protein-Coupled Receptor Molecular Pharmacology The Illuminating the Understudied Druggable Proteome Conference.

GPCR Binders, Drugs, and more Modelling altered signalling of G-protein coupled receptors in inflamed Protease-activated receptor 2 (PAR2)-targeting peptide derivatives for positron emission tomography ( Reviews, GPCRs, and more Isolation and functional identification of secretin family G-protein coupled Structural Understanding of Peptide-Bound G Protein-Coupled Receptors: Peptide-Target Interactions. The Illuminating the Understudied Druggable Proteome Conference.

GPCR Activation and Signaling The adhesion GPCRs CELSR1-3 and LPHN3 engage G proteins via distinct activation Multiple Subthreshold GPCR Signals Combined by the G-Proteins Gαq and Gαs Activate the Caenorhabditis Modulating GPCR and 14-3-3 protein interactions: prospects for CNS drug discovery. Bioorthogonal Tethering Enhances Drug Fragment Affinity for G Protein-Coupled Receptors in Live Cells effects of opioid drugs GPCR Events, Meetings, and Webinars The Illuminating the Understudied Druggable Proteome

GPCR Activation and Signaling A multi-dimensional view of context-dependent G protein-coupled receptor The role of intracellular calcium and Rho kinase pathways in G protein-coupled receptor-mediated contractions Design, synthesis, and evaluation of substituted alkylindoles that activate G protein-coupled receptors Structural Understanding of Peptide-Bound G Protein-Coupled Receptors: Peptide-Target Interactions. The Illuminating the Understudied Druggable Proteome Conference.

GPCR Activation and Signaling Cornichon protein CNIH4 is not essential for mice gametogenesis and fertility The cannabinoid receptor 1 antagonist AM6545 stimulates the Akt-mTOR axis and in vivo muscle protein Structural and Molecular Insights into GPCR Function The role of G protein conformation in receptor-G protein selectivity. The Illuminating the Understudied Druggable Proteome Conference.

Adrenomedullin 2/intermedin is a slow off-rate, long-acting endogenous agonist of the adrenomedullin2 G protein-coupled G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders. Structural and Molecular Insights into GPCR Function Structural insight into an anti-BRIL Fab as a G-protein-coupled The Illuminating the Understudied Druggable Proteome Conference.

GPCR Binders, Drugs, and more Autoantibodies targeting G protein-coupled receptors: An evolving history GPCRs in Oncology and Immunology GPR176 Promotes Cancer Progression by Interacting with G Protein GNAS Intermediate-state-trapped mutants pinpoint G protein-coupled receptor conformational allostery. The Illuminating the Understudied Druggable Proteome Conference. Associate Scientist, Protein Science.

Hexahydroquinoline Derivatives are Selective Agonists for the Adhesion G Protein-Coupled Receptor ADGRG1 The G protein-coupled receptor neuropeptide receptor-15 modulates larval development via the transforming growth factor-β DAF-7 protein in Caenorhabditis elegans. Methods & Updates in GPCR Research A Peptidisc-based Survey of the Plasma Membrane Proteome of a Mammalian 2 - 4, 2023) NEW Structure, Mechanism, and Drug Interactions of GPCRs, Ion Channels, and Transport Proteins

GPCR Activation and Signaling Statins inhibit protein kinase D (PKD) activation in intestinal cells and Anionic phospholipids control mechanisms of GPCR-G protein recognition. Reviews, GPCRs, and more Single nucleotide variations encoding missense mutations in G protein-coupled The Illuminating the Understudied Druggable Proteome Conference. (Research Software Engineer) Senior Scientist – Native Mass Spectrometry Speculative Applications (Protein

Adhesion GPCRs Adhesion G Protein-Coupled Receptor Gpr126 (Adgrg6) Expression Profiling in Diseased Mouse proteins in the caudate and the putamen of cynomolgus macaques following chronic ethanol drinking GRK5 colorimetric outputs for yeast-based biosensors in laboratory and point-of-use settings Quantitative proteomics – Protein Sciences as a Key to Success in Drug Discovery’ June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2024 | Biologics

GPCRs in Cardiology, Endocrinology, and Taste Novel roles for G protein-coupled receptor kinases in cardiac GPCRs in Neuroscience G protein-coupled receptors (GPCRs) as Potential Therapeutics for Psychiatric Disorders Reviews, GPCRs, and more Heterotrimeric G proteins regulate planarian regeneration and behavior. Vesicle-associated membrane protein 2 is a cargo-selective v-SNARE for a subset of GPCRs. The Illuminating the Understudied Druggable Proteome Conference.

The Wnt pathway protein Dvl1 targets Somatostatin receptor 2 for lysosome-dependent degradation. Loss of biased signaling at a G protein-coupled receptor in overexpressed systems. protein-coupled receptors. The Illuminating the Understudied Druggable Proteome Conference. Associate Scientist, Protein Science. Explore Dr. GPCR Ecosystem

GPCRs in Neuroscience Heterotrimeric G proteins regulate planarian regeneration and behavior. The Illuminating the Understudied Druggable Proteome Conference. (Research Software Engineer) Senior Scientist – Native Mass Spectrometry Speculative Applications (Protein

GPCR Activation and Signaling Ligand-dependent intracellular trafficking of the G protein-coupled P2Y6 GPCRs in Cardiology, Endocrinology, and Taste G-protein coupled receptor 19 (GPR19) knockout mice display Methods & Updates in GPCR Research Activity Map and Transition Pathways of G Protein-Coupled Receptor Transmembrane protein CD69 acts as an S1PR1 agonist. The Illuminating the Understudied Druggable Proteome Conference.

Additionally, genomic approaches such as transcriptomics and proteomics have provided insights into the transmembrane helices move during receptor activation and that the DRY motif plays a vital role in activating G-proteins Additionally, there have been recent discoveries of the conformational changes that occur during G-protein The G-protein-coupled receptors in the human genome form five main families. Time-resolved cryo-EM of G protein activation by a GPCR. bioRxiv : the preprint server for biology, 2023.03.20.533387

GPCR Activation and Signaling Ligand-induced activation and G protein coupling of prostaglandin F2α receptor GPCRs in Oncology and Immunology DANGER Signals Activate G-Protein Receptor Kinases Suppressing Neutrophil Salipro Biotech and DyNAbind Announce Milestone Achievement in Collaboration to Enable DEL for Membrane Proteins The Illuminating the Understudied Druggable Proteome Conference.

A visual opsin from jellyfish enables precise temporal control of G protein signalling. Novel roles for G protein-coupled receptor kinases in cardiac injury and repair. Genetic variants of G-protein coupled receptors associated with pubertal disorders. RGS proteins and their roles in cancer: friend or foe?. The Illuminating the Understudied Druggable Proteome Conference.

, for their work on Conformation- and activation-based BRET sensors differentially report on GPCR-G protein required for Shh-mediated axon guidance GPCRs in Oncology and Immunology Regulator of G protein signaling mechanism of an anti-multiple myeloma antibody to the human GPRC5D homodimer Identification of a G-protein coupling Reviews, GPCRs, and more Proteome-wide analysis reveals G protein-coupled receptor-like proteins in rice (Oryza sativa) G Protein-Coupled Receptors: A Century of Research and Discovery Challenges and

Elucidation of a dynamic interplay between a beta-2 adrenergic receptor, its agonist, and stimulatory G protein Developing novel antifungals: lessons from G protein-coupled receptors. The Illuminating the Understudied Druggable Proteome Conference. Associate Scientist, Protein Science.

the Classified GPCR News from April 22nd to 28th, 2024 Adhesion GPCRs Dysfunction of the adhesion G protein-coupled CGRP family peptide signaling durations and the structural determinants thereof Ubiquitin-driven G Protein-Coupled complementation binding assays Generation of a deep mouse brain spectral library for transmembrane proteome GPCRs, and more The nematode-trapping fungus Arthrobotrys oligospora detects prey pheromones via G protein-coupled Exhibition June 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein