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

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.

Publication types

  • Review

MeSH terms

  • Animals
  • Arrestins / metabolism*
  • Humans
  • Phosphorylation
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction*


  • Arrestins
  • Receptors, G-Protein-Coupled