Department of Pharmacology, School of Medicine, Case Western Reserve University, Cleveland, OH 44106-4965, USA.
Trends Biochem Sci. 2010 Nov;35(11):595-600. doi: 10.1016/j.tibs.2010.05.002. Epub 2010 Jun 9.
Oligomerization is a general characteristic of cell membrane receptors that is shared by G protein-coupled receptors (GPCRs) together with their G protein partners. Recent studies of these complexes, both in vivo and in purified reconstituted forms, unequivocally support this contention for GPCRs, perhaps with only rare exceptions. As evidence has evolved from experimental cell lines to more relevant in vivo studies and from indirect biophysical approaches to well defined isolated complexes of dimeric receptors alone and complexed with G proteins, there is an expectation that the structural basis of oligomerization and the functional consequences for membrane signaling will be elucidated. Oligomerization of cell membrane receptors is fully supported by both thermodynamic calculations and the selectivity and duration of signaling required to reach targets located in various cellular compartments.
寡聚化是细胞膜受体的一个普遍特征,G 蛋白偶联受体 (GPCR)与其 G 蛋白伴侣共同具有这一特征。最近对这些复合物的体内和纯化重建形式的研究,明确支持了这一观点,也许只有极少数例外。随着证据从实验细胞系发展到更相关的体内研究,从间接的生物物理方法发展到单独的二聚体受体及其与 G 蛋白复合物的明确定义的分离复合物,人们期望寡聚化的结构基础和对膜信号转导的功能后果将被阐明。细胞膜受体的寡聚化完全得到热力学计算和信号转导的选择性和持续时间的支持,这些信号转导需要到达位于不同细胞区室的靶标。