Deupi Xavier, Kobilka Brian
Department of Molecular and Cellular Physiology, Stanford University School of Medicine, Stanford, California 94305, USA.
Adv Protein Chem. 2007;74:137-66. doi: 10.1016/S0065-3233(07)74004-4.
G protein-coupled receptors (GPCRs) mediate responses to hormones and neurotransmitters, as well as the senses of sight, smell, and taste. These remarkably versatile signaling molecules respond to structurally diverse ligands. Many GPCRs couple to multiple G protein subtypes, and several have been shown to activate G protein-independent signaling pathways. Drugs acting on GPCRs exhibit efficacy profiles that may differ for different signaling cascades. The functional plasticity exhibited by GPCRs can be attributed to structural flexibility and the existence of multiple ligand-specific conformational states. This chapter will review our current understanding of the mechanism by which agonists bind and activate GPCRs.
G蛋白偶联受体（GPCRs）介导对激素和神经递质的反应，以及视觉、嗅觉和味觉。这些极其通用的信号分子对结构多样的配体作出反应。许多GPCRs与多种G蛋白亚型偶联，并且已经证明有几种会激活不依赖G蛋白的信号通路。作用于GPCRs的药物表现出的疗效特征可能因不同的信号级联反应而异。GPCRs表现出的功能可塑性可归因于结构灵活性和多种配体特异性构象状态的存在。本章将综述我们目前对激动剂结合并激活GPCRs机制的理解。
