Tobin Andrew B, Butcher Adrian J, Kong Kok Choi
Department of Cell Physiology and Pharmacology, University of Leicester, LE1 9HN, UK.
Trends Pharmacol Sci. 2008 Aug;29(8):413-20. doi: 10.1016/j.tips.2008.05.006. Epub 2008 Jul 6.
It is now established that most of the approximately 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.
现已确定，在大约800种G蛋白偶联受体（GPCRs）中，大多数受体通过磷酸化作用进行调节，这一过程会导致抑制蛋白的募集，进而引起受体脱敏以及激活依赖于抑制蛋白的过程。然而，这种GPCR调节的普遍观点并不能为组织特异性GPCR信号传导的控制提供充分的机制。在此，我们回顾相关证据，事实上，GPCR磷酸化是一个灵活且动态的调节过程，其中GPCR以一种独特的方式被磷酸化，这种方式与表达该受体的细胞类型相关。在这种情况下，磷酸化提供了一种调节GPCR信号转导结果的机制，该机制可进行调整以满足特定的生理作用。
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