期刊
TRENDS IN PHARMACOLOGICAL SCIENCES
卷 40, 期 4, 页码 236-239出版社
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2019.02.005
关键词
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GPCRs couple to intracellular transducer proteins, which reciprocally closes the extracellular ligand binding pocket, a process called allosteric coupling. Biased agonists preferentially stimulate receptor coupling to specific signaling pathways. Here, we postulate that agonists with extended binding modes selectively interfere with binding pocket closure, which results in divergent allosteric coupling, eventually leading to ligand bias.
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