Tobin_2008_Br.J.Pharmacol_153 Suppl 1_S167

Reference

Title : G-protein-coupled receptor phosphorylation: where, when and by whom - Tobin_2008_Br.J.Pharmacol_153 Suppl 1_S167
Author(s) : Tobin AB
Ref : British Journal of Pharmacology , 153 Suppl 1 :S167 , 2008
Abstract :

Almost all G-protein coupled receptors (GPCRs) are regulated by phosphorylation and this process is a key event in determining the signalling properties of this receptor super-family. Receptors are multiply phosphorylated at sites that can occur throughout the intracellular regions of the receptor. This diversity of phospho-acceptor sites together with a lack of consensus phosphorylation sequences has led to the suggestion that the precise site of phosphorylation is not important in the phosphorylation-dependent regulation of GPCR function but rather it is the increase in bulk negative charge of the intracellular face of the receptor which is the significant factor. This review investigates the possibility that the multi-site nature of GPCR phosphorylation reflects the importance of specific phosphorylation events which mediate distinct signalling outcomes. In this way receptor phosphorylation may provide for a flexible regulatory mechanism that can be tailored in a tissue specific manner to regulate physiological processes. By understanding the flexible nature of GPCR phosphorylation if may be possible to develop agonists or allosteric modulators that promote a subset of phosphorylation events on the target GPCR and thereby restrict the action of the drug to a particular receptor mediated signalling response.

PubMedSearch : Tobin_2008_Br.J.Pharmacol_153 Suppl 1_S167
PubMedID: 18193069

Related information

Citations formats

Tobin AB (2008)
G-protein-coupled receptor phosphorylation: where, when and by whom
British Journal of Pharmacology 153 Suppl 1 :S167

Tobin AB (2008)
British Journal of Pharmacology 153 Suppl 1 :S167