Milligan Graeme
Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, UK.
Biochim Biophys Acta. 2007 Apr;1768(4):825-35. doi: 10.1016/j.bbamem.2006.09.021. Epub 2006 Sep 30.
The belief that G protein-coupled receptors exist and function as monomeric, non-interacting species has been largely supplanted in recent years by evidence, derived from a range of approaches, that indicate they can form dimers and/or higher-order oligomeric complexes. Key roles for receptor homo-dimerisation include effective quality control of protein folding prior to plasma membrane delivery and interactions with hetero-trimeric G proteins. Growing evidence has also indicated the potential for many co-expressed G protein-coupled receptors to form hetero-dimers/oligomers. The relevance of this to physiology and function is only beginning to be unravelled but may offer great potential for more selective therapeutic intervention.
近年来，一系列研究证据表明G蛋白偶联受体能够形成二聚体和/或更高阶的寡聚复合物，这在很大程度上取代了此前认为G蛋白偶联受体以单体、非相互作用形式存在并发挥功能的观点。受体同二聚化的关键作用包括在质膜转运之前对蛋白质折叠进行有效的质量控制以及与异源三聚体G蛋白的相互作用。越来越多的证据还表明，许多共表达的G蛋白偶联受体有形成异二聚体/寡聚体的可能性。其与生理学和功能的相关性才刚刚开始被揭示，但可能为更具选择性的治疗干预提供巨大潜力。
