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Showing 1–16 of 16 results
Advanced filters: Author: Dmitry B. Veprintsev Clear advanced filters

  • Nonselective engagement of GPCR signaling pathways by GPCR-targeting drugs can reduce treatment efficacy and cause side effects. The authors show that signaling selectivity in CB2R can be tuned by reshaping allosteric networks, offering insights for more precise therapies.

    • Adrian Morales-Pastor
    • Tamara Miljuš
    • Jana Selent
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-14

  • Tetrahydrocannabinol (THC) analogs target the cannabinoid receptor CB1 for therapeutic and psychoactive effects. Here, the authors determine spatiotemporal ligand interactions critical for potency, efficacy, off-rates and drug design.

    • Thor S. Thorsen
    • Yashraj Kulkarni
    • David E. Gloriam
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-13

  • The cellular functions of arrestins are determined in part by the pattern of phosphorylation on the G protein-coupled receptors (GPCRs) to which arrestins bind. Here, authors use a library of synthetic phosphopeptide analogues of the GPCR rhodopsin C-terminus and determine the ability of these peptides to bind and activate arrestins using a variety of biochemical and biophysical methods.

    • Daniel Mayer
    • Fred F. Damberger
    • Dmitry B. Veprintsev
    ResearchOpen Access
    Nature Communications
    Volume: 10, P: 1-14

  • Extensive mutant cycle analysis provides a map of the residues that contribute to stability and activation-associated conformational dynamics of the Gαi1 protein in nucleotide-bound states and in complex with the G protein–coupled receptor rhodopsin.

    • Dawei Sun
    • Tilman Flock
    • Dmitry B Veprintsev
    Research
    Nature Structural & Molecular Biology
    Volume: 22, P: 686-694

  • Smells are detected in the nose by odorant molecules binding to a specific G protein-coupled receptor on the cell surface. Here, authors have determined the atomic structure of a receptor bound to an odorant molecule that showing how the odorant binds and activates the receptor.

    • Anastasiia Gusach
    • Yang Lee
    • Christopher G. Tate
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-12

  • A new crystal structure of BtuCD, a bacterial ABC transporter that uses ATP hydrolysis to drive vitamin B12 uptake, bound to an AMP-PNP nucleotide, completes the structural elucidation of intermediates in the transport cycle and reveals how ATP accelerates transport.

    • Vladimir M Korkhov
    • Samantha A Mireku
    • Kaspar P Locher
    Research
    Nature Structural & Molecular Biology
    Volume: 21, P: 1097-1099

  • Comparative analysis of inactive/active-state structures reveals molecular mechanistic maps of activation of the major GPCR classes. The findings and new approaches lay the foundation for targeted receptor-function studies and drugs with desired modalities.

    • Alexander S. Hauser
    • Albert J. Kooistra
    • David E. Gloriam
    ResearchOpen Access
    Nature Structural & Molecular Biology
    Volume: 28, P: 879-888

  • Although several X-ray crystal structures of G protein-coupled receptors (GPCRs) have been reported, relatively little is known about the conformational dynamics of these important membrane proteins; here, the authors used NMR spectroscopy to monitor the conformational changes that occur in the turkey β1-adrenergic receptor in the presence of antagonists, partial agonists, and full agonists.

    • Shin Isogai
    • Xavier Deupi
    • Stephan Grzesiek
    Research
    Nature
    Volume: 530, P: 237-241

  • Beta-arrestins play central roles in the mechanisms regulating GPCR signalling and trafficking. Here the authors identify a selective inhibitor of the interaction between β-arrestin and the β2-adaptin subunit of the clathrin adaptor protein AP-2, which they use to dissect the role of the β-arrestin/β2-adaptin interaction in GPCR signalling.

    • Alexandre Beautrait
    • Justine S. Paradis
    • Michel Bouvier
    ResearchOpen Access
    Nature Communications
    Volume: 8, P: 1-16

  • β-Catenin can be oncogenic but finding inhibitors has been a challenge. Here, five compounds are identified, which attenuate transcriptional β-catenin outputs in colorectal cancer cells, and the response to one of them is shown to require an intrinsically labile α-helix next to the BCL9-binding site in β-catenin.

    • Marc de la Roche
    • Trevor J. Rutherford
    • Mariann Bienz
    ResearchOpen Access
    Nature Communications
    Volume: 3, P: 1-10

  • There are ∼800 human GPCRs and 16 different Gα proteins; this study revealed the molecular details of Gα activation by GPCRs and suggests that a universal activation mechanism governs Gα activation—the details of this mechanism can explain how the GPCR–Gα system diversified rapidly, while conserving the allosteric activation mechanism.

    • Tilman Flock
    • Charles N. J. Ravarani
    • M. Madan Babu
    Research
    Nature
    Volume: 524, P: 173-179

  • Stoddart et al. propose rational design of a covalent and selective ligand probe to fluorescently label GPCR in transiently transfected and endogenous systems. Using the adenosine A2A receptor as a model system, they show fluorescent labelling in an endogenous system, without impeding access to the orthosteric binding site. This study is useful to selectively and non-invasively study localisation and functions of GPCRs.

    • Leigh A. Stoddart
    • Nicholas D. Kindon
    • Barrie Kellam
    ResearchOpen Access
    Communications Biology
    Volume: 3, P: 1-9