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时间: 2023-10-02 16:05:03 浏览: 135
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Title: The Structural Basis for G Protein-Coupled Receptor Activation and Inactivation
Authors: Tatsuya Takemoto, Hiroyuki Kusano-Arai, Takuya Kobayashi, Koichi Tamura, Osamu Nureki
Journal: Journal of Chemical Information and Modeling
DOI: 10.1021/acs.jcim.1c00679
Abstract:
G protein-coupled receptors (GPCRs) are one of the most important drug targets, and they play a critical role in signaling pathways involved in various physiological processes. The ligand binding to GPCRs triggers conformational changes that lead to the activation of downstream signaling pathways. In this review, we summarize recent structural studies on the activation and inactivation mechanisms of GPCRs, focusing on the crystal structures of active and inactive states and the conformational changes that occur upon ligand binding and G protein coupling. We also discuss the implications of these structural studies for drug development targeting GPCRs.
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