Regulation of G Protein-coupled Receptor Kinase

Abstract: G protein-coupled receptor kinase (GRK) specifically phosphorylate the agonist-activated form of G protein-coupled receptor (GPCR)， raising its desensitization and then terminating the GPCR-induced signaling. Upon the discovery of GRK family since mid-1980s， it's desired for understanding the biochemical and molecular mechanism of regulation of the GPCR responsiveness. Recent studies demonstrated that the function of GRK is highly regulated， and in this manner regulates the responsiveness of GPCR， among those seven have been identified. The regulating mechanism of the GRK function could be understood in two aspects: (1) subcellular localization and the regulation of GRK kinase activity， including the interaction with GPCR， G protein， phospholipids， Ca²⁺-binding protein， PKC， MAPK， and caveolin; (2) the regulation of GRK expression level in correlation with some diseases， such as cardiovascular disease， hypertension， and inflammation.

CSTR: 32200.14.cjcb.2004.05.0016