Lohse M J, Hein P, Hoffmann C, Nikolaev V O, Vilardaga J-P, Bünemann M
Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany.
Br J Pharmacol. 2008 Mar;153 Suppl 1(Suppl 1):S125-32. doi: 10.1038/sj.bjp.0707656. Epub 2008 Jan 14.
G-protein-coupled receptors (GPCRs) are the largest group of cell surface receptors. They are stimulated by a variety of stimuli and signal to different classes of effectors, including several types of ion channels and second messenger-generating enzymes. Recent technical advances, most importantly in the optical recording with energy transfer techniques--fluorescence and bioluminescence resonance energy transfer, FRET and BRET--, have permitted a detailed kinetic analysis of the individual steps of the signalling chain, ranging from ligand binding to the production of second messengers in intact cells. The transfer of information, which is initiated by ligand binding, triggers a signalling cascade that displays various rate-controlling steps at different levels. This review summarizes recent findings illustrating the speed and the complexity of this signalling system.
G蛋白偶联受体（GPCRs）是最大的细胞表面受体家族。它们受到多种刺激，并向不同类型的效应器发出信号，包括几种离子通道和产生第二信使的酶。最近的技术进步，最重要的是在采用能量转移技术——荧光共振能量转移（FRET）和生物发光共振能量转移（BRET）的光学记录方面的进展，使得对信号转导链各个步骤进行详细的动力学分析成为可能，这些步骤涵盖从配体结合到完整细胞中第二信使的产生。由配体结合引发的信息传递会触发一个信号级联反应，该反应在不同水平上呈现出各种速率控制步骤。本综述总结了近期的研究发现，阐明了该信号系统的速度和复杂性。
