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Showing 1–4 of 4 results
Advanced filters: Author: Anne Grahl Clear advanced filters

  • The β1-adrenergic receptor (β1AR) contains empty cavities in its preactive conformation, which disappear in the active one. Now, using X-ray crystallography of xenon-derivatized β1AR crystals, a cavity has been shown to be in contact with the cholesterol-binding pocket. Monitoring the binding of a cholesterol analogue in solution has explained the function of cholesterol as a negative allosteric modulator of β1AR.

    • Layara Akemi Abiko
    • Raphael Dias Teixeira
    • Stephan Grzesiek
    Research
    Nature Chemistry
    Volume: 14, P: 1133-1141

  • Signal transmission and regulation of G-protein-coupled receptors (GPCRs) by ligands occurs via modulation of complex conformational equilibria. Here authors quantify these equilibria and their dynamics in the β1-adrenergic receptor in its apo form and seven ligand complexes using NMR.

    • Anne Grahl
    • Layara Akemi Abiko
    • Stephan Grzesiek
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-13

  • Recent advances in structural biology techniques and computational simulations have enhanced our understanding of the conformational dynamics of G protein-coupled receptors and their interactions with ligands. This Review highlights how such advances may be used in the discovery and optimization of drugs that target G protein-coupled receptors, focusing on three categories: allosteric modulators, biased ligands, and bivalent and bitopic compounds.

    • Paolo Conflitti
    • Edward Lyman
    • Vittorio Limongelli
    Reviews
    Nature Reviews Drug Discovery
    Volume: 24, P: 251-275