Dimerization in GPCR mobility and signaling

Dimerization in GPCR mobility and signaling
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DOI:
10.1016/j.coph.2009.10.007
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发表时间:
2010-02-01
影响因子:
4
通讯作者:
Lohse, Martin J.
Lohse, Martin J.
中科院分区:
医学3区
文献类型:
--
作者:
Lohse, Martin J.

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许多类型的细胞表面以及细胞内DNA结合受体存在并作为二聚体起作用;同源二聚体或异源二聚体的形成似乎不仅提供激动剂诱导的活化的分子机制,而且增加配体识别的特异性和下游信号传导的多功能性。长期以来,G蛋白偶联受体(GPCR)被认为是一个例外,但近年来积累了大量证据表明GPCR也可以形成二聚体,尽管在生理条件下它们实际上何时何地形成二聚体还远未确定。GPCR的二聚化通常似乎不是配体识别或信号传导所需的。然而,二聚化可能会影响受体在细胞表面和细胞内运输的迁移率,并可能参与和影响它们的信号传导功能。
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.