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Trends Pharmacol Sci. 2008 Aug;29(8):413-20. doi: 10.1016/j.tips.2008.05.006. Epub 2008 Jul 6.

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

Author information

1
Department of Cell Physiology and Pharmacology, University of Leicester, LE1 9HN, UK. tba@le.ac.uk

Abstract

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.

PMID:
18606460
PMCID:
PMC2880250
DOI:
10.1016/j.tips.2008.05.006
[Indexed for MEDLINE]
Free PMC Article

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