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Location, location, location ... site-specific GPCR phosphorylation offers a mechanism for cell-type-specific signalling

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TRENDS IN PHARMACOLOGICAL SCIENCES
卷 29, 期 8, 页码 413-420

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ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2008.05.006

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It is now established that most of the similar to 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.

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