Torrecilla_2006_Curr.Pharm.Des_12_1797

Reference

Title : Co-ordinated covalent modification of G-protein coupled receptors - Torrecilla_2006_Curr.Pharm.Des_12_1797
Author(s) : Torrecilla I , Tobin AB
Ref : Curr Pharm Des , 12 :1797 , 2006
Abstract :

The G-protein coupled receptor (GPCR) gene family represents one of the largest families in the mammalian genome. The flexibility of signalling and widespread tissue distribution of these receptors has allowed GPCRs to be employed in the physiological regulation of nearly all biological functions. This, coupled with the fact that it is possible to chemically produce highly specific ligands to these receptors have made GPCRs attractive targets for pharmacological intervention in a wide variety of disease states. When targeting GPCRs in therapeutic drug design it is traditional, and eminently sensible, to focus on ligands that will provide agonism, antagonism or allosteric modulation. However, as more is understood of the mechanisms that regulate GPCRs, and in particular the dynamic covalent modifications that might endow tissue specific functions, then these regulatory processes may provide alternative targets for GPCR drug discovery. In this review we consider three of the covalent modifications which are considered to regulate the function of GPCRs namely; receptor phosphorylation, palmitoylation and ubiquitination. In particular, we will describe the mechanisms of modification, the functional consequences and the relationship between these three covalent modification events.

PubMedSearch : Torrecilla_2006_Curr.Pharm.Des_12_1797
PubMedID: 16712489

Related information

Citations formats

Torrecilla I, Tobin AB (2006)
Co-ordinated covalent modification of G-protein coupled receptors
Curr Pharm Des 12 :1797

Torrecilla I, Tobin AB (2006)
Curr Pharm Des 12 :1797