Targeting cryptic allosteric sites of G protein-coupled receptors as a novel strategy for biased drug discovery

G protein-coupled receptors (GPCRs) represent the largest family of membrane receptors and are highly effective targets for therapeutic drugs. GPCRs couple different downstream effectors, including G proteins (such as Gi/o, Gs, G12, and Gq) and β-arrestins (such as β-arrestin 1 and β-arrestin 2) to...

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Bibliographic Details

Published in:	Pharmacological Research
Main Authors:	Xin Qiao, Xiaolong Li, Mingyang Zhang, Ning Liu, Yanmei Wu, Shaoyong Lu, Ting Chen
Format:	Article
Language:	English
Published:	Elsevier 2025-02-01
Subjects:	G protein-coupled receptors Biased signaling Cryptic allosteric sites Allosteric modulators Drug design
Online Access:	http://www.sciencedirect.com/science/article/pii/S104366182400519X