Institute of Pharmacology and Toxicology, Würzburg, Germany.
Curr Opin Pharmacol. 2010 Feb;10(1):53-8. doi: 10.1016/j.coph.2009.10.007. Epub 2009 Nov 10.
Many types of cell surface as well as intracellular DNA-binding receptors exist and function as dimers; formation of homodimers or heterodimers appears to not only provide molecular mechanisms for agonist-induced activation but also increase specificity of ligand recognition and versatility of downstream signaling. G-protein-coupled receptors (GPCRs) were long thought to be an exception, but in recent years a lot of evidence has accumulated that GPCRs also can form dimers, even though it is far from certain when and where they actually do so under physiological conditions. Dimerization of GPCRs does not generally seem to be required for ligand recognition or signaling. However, dimerization may serve to affect receptor mobility at the cell surface and in intracellular trafficking, and may be involved in and affect their signaling functions.
存在许多类型的细胞表面和细胞内 DNA 结合受体，它们作为二聚体发挥作用；形成同源二聚体或异源二聚体不仅为激动剂诱导的激活提供了分子机制，而且增加了配体识别的特异性和下游信号转导的多功能性。G 蛋白偶联受体 (GPCR) 长期以来被认为是一个例外，但近年来有大量证据表明 GPCR 也可以形成二聚体，尽管在生理条件下它们实际上何时以及在何处形成二聚体还远未确定。GPCR 二聚化通常似乎不是配体识别或信号转导所必需的。然而，二聚化可能有助于影响细胞表面和细胞内运输过程中的受体流动性，并可能参与和影响它们的信号转导功能。
