An allosteric modulator binds to a conformational hub in the β<sub>2</sub> adrenergic receptor

June 1st, 2020 by Xiangyu Liu

Nature Chemical Biology, Published online: 01 June 2020; doi:10.1038/s41589-020-0549-2

A negative allosteric modulator of the G-protein-coupled receptor β2-adrenergic receptor binds to a membrane-facing surface adjacent to a molecular switch for receptor activation, and its binding disrupts a water-mediated polar network stabilizing an inactive switch conformation.
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