Milligan Graeme
Molecular Pharmacology Group, Davidson Building, University of Glasgow, Glasgow G12 8QQ Scotland, UK.
Mol Pharmacol. 2004 Jul;66(1):1-7. doi: 10.1124/mol.104.000497..
It is now generally accepted that G protein-coupled receptors (GPCRs) can exist as dimers or as part of larger oligomeric complexes. Increasing evidence suggests that a dimer is the minimal functional structure, but considerable variation exists between reports of the effects of agonist ligands on quaternary structure. Many studies have intimated the existence of heterodimeric GPCR pairings. Key questions that remain to be addressed effectively include the prevalence and relevance of these in native tissues and the implications of heterodimerization for pharmacology and, potentially, for drug design.
目前普遍认为，G蛋白偶联受体（GPCRs）可以以二聚体形式存在，或作为更大的寡聚复合物的一部分。越来越多的证据表明，二聚体是最小的功能结构，但激动剂配体对四级结构的影响报告之间存在相当大的差异。许多研究暗示了异源二聚体GPCR配对的存在。有待有效解决的关键问题包括这些在天然组织中的普遍性和相关性，以及异源二聚化对药理学以及潜在的药物设计的影响。
