Location, location, location...site-specific GPCR phosphorylation offers a mechanism for cell-type-specific signalling.
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.
Tobin
Andrew B
AB
Department of Cell Physiology and Pharmacology, University of Leicester, LE1 9HN, UK. tba@le.ac.uk
Butcher
Adrian J
AJ
Kong
Kok Choi
KC
D000818:Animals; D019390:Arrestins / Q000378:metabolism*; D006801:Humans; D010766:Phosphorylation; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*; D015398:Signal Transduction
D019390:Arrestins; D043562:Receptors, G-Protein-Coupled