Weis William I, Kobilka Brian K
Department of Molecular & Cellular Physiology, Stanford University School of Medicine, USA.
Curr Opin Struct Biol. 2008 Dec;18(6):734-40. doi: 10.1016/j.sbi.2008.09.010. Epub 2008 Nov 17.
G-protein-coupled receptors (GPCRs) are the largest family of eukaryotic plasma membrane receptors, and are responsible for the majority of cellular responses to external signals. GPCRs share a common architecture comprising seven transmembrane (TM) helices. Binding of an activating ligand enables the receptor to catalyze the exchange of GTP for GDP in a heterotrimeric G protein. GPCRs are in a conformational equilibrium between inactive and activating states. Crystallographic and spectroscopic studies of the visual pigment rhodopsin and two beta-adrenergic receptors have defined some of the conformational changes associated with activation.
G蛋白偶联受体（GPCRs）是真核细胞质膜受体中最大的家族，负责细胞对外部信号的大部分反应。GPCRs具有共同的结构，包括七个跨膜（TM）螺旋。激活配体的结合使受体能够催化异源三聚体G蛋白中GTP与GDP的交换。GPCRs在失活状态和激活状态之间处于构象平衡。对视觉色素视紫红质和两种β-肾上腺素能受体的晶体学和光谱学研究已经确定了一些与激活相关的构象变化。
