Department of Pharmacology, University of Minnesota, Minneapolis, MN 55455-0217, USA.
IUBMB Life. 2010 Feb;62(2):112-9. doi: 10.1002/iub.293.
Agonist-selective signaling or ligand-biased signaling of G protein-coupled receptor (GPCR) has become the focus of an increasing number of laboratories. The principle of this concept is that agonist possesses different abilities to activate different signaling pathways. Current review summarizes the observations of agonist-selective signaling of various GPCRs, indicating the significance of agonist-selective signaling in biological processes. In addition, current review also provides an overview on how agonist-selective signaling is initiated. Especially, the relationship between GPCR-G protein interaction and GPCR-beta-arrestin interaction is discussed in depth.
激动剂选择性信号转导或 G 蛋白偶联受体 (GPCR) 的配体偏倚信号转导已成为越来越多实验室的研究重点。这一概念的原理是,激动剂具有激活不同信号通路的不同能力。本综述总结了各种 GPCR 的激动剂选择性信号转导的观察结果,表明了激动剂选择性信号转导在生物过程中的重要性。此外,本综述还概述了激动剂选择性信号转导的起始方式。特别是,深入讨论了 GPCR-G 蛋白相互作用与 GPCR-β-arrestin 相互作用之间的关系。