Kroeger Karen M, Pfleger Kevin D G, Eidne Karin A
Western Australian Institute for Medical Research, Centre for Medical Research, University of Western Australia, Sir Charles Gairdner Hospital, Hospital Avenue, Nedlands, 6009, Perth, WA, Australia.
Front Neuroendocrinol. 2003 Dec;24(4):254-78. doi: 10.1016/j.yfrne.2003.10.002.
Protein-protein interactions are fundamental processes for many biological systems including those involving the superfamily of G-protein coupled receptors (GPCRs). A growing body of biochemical and functional evidence supports the existence of GPCR-GPCR homo- and hetero-oligomers. In particular, hetero-oligomers can display pharmacological and functional properties distinct from those of the homodimer or oligomer thus adding another level of complexity to how GPCRs are activated, signal and traffick in the cell. Dimerization may also play a role in influencing the activity of agonists and antagonists. We are only beginning to unravel how and why such complexes are formed, the functional implications of which will have an enormous impact on GPCR biology. Future research that studies GPCRs as dimeric or oligomeric complexes will enhance not only our understanding of GPCRs in cellular function but will also be critical for novel drug design and improved treatment of the vast array of GPCR-related conditions.
蛋白质-蛋白质相互作用是许多生物系统的基本过程，包括那些涉及G蛋白偶联受体（GPCR）超家族的系统。越来越多的生化和功能证据支持GPCR-GPCR同型和异型寡聚体的存在。特别是，异型寡聚体可以表现出与同型二聚体或寡聚体不同的药理学和功能特性，从而为GPCR在细胞中的激活、信号传导和运输方式增加了另一层复杂性。二聚化也可能在影响激动剂和拮抗剂的活性方面发挥作用。我们才刚刚开始弄清楚这些复合物是如何形成的以及为何形成，其功能意义将对GPCR生物学产生巨大影响。未来将GPCR作为二聚体或寡聚体复合物进行研究的工作，不仅会增进我们对GPCR在细胞功能中的理解，对于新型药物设计以及改善大量与GPCR相关病症的治疗也至关重要。
