GPCRs and Signal Transducers: Interaction Stoichiometry.

GPCRs and Signal Transducers: Interaction Stoichiometry.
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DOI:
10.1016/j.tips.2018.04.002
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发表时间:
2018-07
影响因子:
13.8
通讯作者:
Gurevich EV
Gurevich EV
中科院分区:
医学1区
文献类型:
--
作者:
Gurevich VV;Gurevich EV

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直到20世纪90年代末,A类G蛋白偶联受体(GPCR)仍被认为具有单体功能。然后,间接证据表明,它们可能内化,甚至作为二聚体发出信号,沿着C类GPCR是强制性二聚体的证据。GPCR及其更大的结合伴侣的晶体结构与两种受体可能参与单个G蛋白、GRK或抑制蛋白的想法一致。然而,最近的生物物理,生物化学和结构的证据总是表明,一个单一的GPCR结合G蛋白,GRKs和arrestins。在这里,我们回顾现有的证据GPCR与信号转导的化学计量相互作用,并讨论潜在的生物学作用的A类GPCR寡聚体,包括建议的同源和异源二聚体。
Until the late 1990s class A G protein-coupled receptors (GPCRs) were believed to function as monomers. Then indirect evidence that they might internalize or even signal as dimers has emerged, along with proof that class C GPCRs are obligatory dimers. Crystal structures of GPCRs and their much larger binding partners were consistent with the idea that two receptors might engage a single G protein, GRK, or arrestin. However, recent biophysical, biochemical, and structural evidence invariably suggested that a single GPCR binds G proteins, GRKs, and arrestins. Here we review existing evidence of the stoichiometry of GPCR interactions with signal transducers and discuss potential biological roles of class A GPCR oligomers, including proposed homo- and heterodimers.
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