Gether U
Department of Medical Physiology, Panum Institute, University of Copenhagen, Denmark.
Endocr Rev. 2000 Feb;21(1):90-113. doi: 10.1210/edrv.21.1.0390.
G protein-coupled, seven-transmembrane segment receptors (GPCRs or 7TM receptors), with more than 1000 different members, comprise the largest superfamily of proteins in the body. Since the cloning of the first receptors more than a decade ago, extensive experimental work has uncovered multiple aspects of their function and challenged many traditional paradigms. However, it is only recently that we are beginning to gain insight into some of the most fundamental questions in the molecular function of this class of receptors. How can, for example, so many chemically diverse hormones, neurotransmitters, and other signaling molecules activate receptors believed to share a similar overall tertiary structure? What is the nature of the physical changes linking agonist binding to receptor activation and subsequent transduction of the signal to the associated G protein on the cytoplasmic side of the membrane and to other putative signaling pathways? The goal of the present review is to specifically address these questions as well as to depict the current awareness about GPCR structure-function relationships in general.
G蛋白偶联的七跨膜片段受体（GPCRs或7TM受体）有1000多个不同成员，是体内最大的蛋白质超家族。自十多年前首次克隆出这类受体以来，大量实验工作揭示了其功能的多个方面，并对许多传统范式提出了挑战。然而，直到最近我们才开始深入了解这类受体分子功能中一些最基本的问题。例如，如此多化学性质各异的激素、神经递质和其他信号分子如何激活被认为具有相似整体三级结构的受体？将激动剂结合与受体激活以及随后将信号转导至膜细胞质侧相关G蛋白和其他假定信号通路的物理变化的本质是什么？本综述的目的是专门解决这些问题，并总体描述目前对GPCR结构-功能关系的认识。
