G蛋白偶联受体介导的异源三聚体G蛋白激活

Heterotrimeric G protein activation by G-protein-coupled receptors.

作者信息

Oldham William M, Hamm Heidi E

机构信息

Department of Pharmacology, Vanderbilt University School of Medicine, 442 Robinson Research Building, 2222 Pierce Avenue, Nashville, TN 37232-6600, USA.

出版信息

Nat Rev Mol Cell Biol. 2008 Jan;9(1):60-71. doi: 10.1038/nrm2299.

DOI:10.1038/nrm2299

PMID:18043707

Abstract

Heterotrimeric G proteins have a crucial role as molecular switches in signal transduction pathways mediated by G-protein-coupled receptors. Extracellular stimuli activate these receptors, which then catalyse GTP-GDP exchange on the G protein alpha-subunit. The complex series of interactions and conformational changes that connect agonist binding to G protein activation raise various interesting questions about the structure, biomechanics, kinetics and specificity of signal transduction across the plasma membrane.

摘要

异源三聚体G蛋白作为分子开关在G蛋白偶联受体介导的信号转导途径中起着关键作用。细胞外刺激激活这些受体，然后这些受体催化G蛋白α亚基上的GTP-GDP交换。将激动剂结合与G蛋白激活联系起来的一系列复杂的相互作用和构象变化引发了关于跨质膜信号转导的结构、生物力学、动力学和特异性的各种有趣问题。