Location, location, location...site-specific GPCR phosphorylation offers a mechanism for cell-type-specific signalling.
Location, location, location...site-specific GPCR phosphorylation offers a mechanism for cell-type-specific signalling.
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DOI：
10.1016/j.tips.2008.05.006
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发表时间：
2008-08
影响因子：
13.8
通讯作者：
Kong KC
中科院分区：
文献类型：
--
作者：
Tobin AB;Butcher AJ;Kong KC
现已证实，∼800G蛋白偶联受体(GPCR)中的大多数受磷酸化调控，该过程导致抑制素的募集，导致受体脱敏和激活arrestin依赖的过程。然而，这种对GPCR调控的普遍看法并没有为组织特异性GPCR信号的控制提供足够的机制。在这里，我们回顾了GPCR磷酸化实际上是一个灵活和动态的调节过程的证据，在这个过程中，GPCRs以一种独特的方式被磷酸化，这种方式与受体表达的细胞类型有关。在这种情况下，磷酸化提供了一种调节GPCRs信号转导结果的机制，可以根据特定的生理角色进行定制。
It is now established that most of the ∼800 G-protein-coupled receptors (GPCRs) are regulated by phosphorylation in a process that results in the recruitment of arrestins, leading to receptor desensitization and the activation of arrestin-dependent processes. This generalized view of GPCR regulation, however, does not provide an adequate mechanism for the control of tissue-specific GPCR signalling. Here, we review the evidence that GPCR phosphorylation is, in fact, a flexible and dynamic regulatory process in which GPCRs are phosphorylated in a unique manner that is associated with the cell type in which the receptor is expressed. In this scenario, phosphorylation offers a mechanism of regulating the signalling outcome of GPCRs that can be tailored to meet a specific physiological role.