G protein-coupled receptor kinase 2 (GRK2) plays a key role in determi
ning the rate and extent of G protein-coupled receptor (GPCR) desensit
ization and resensitization, Recent data indicate that GRK2 activity,
subcellular distribution and expression are tightly regulated. The imp
ortant physiological function of GRK2 as a modulator of the efficacy o
f GPCR signal transduction systems is exemplified by its relevance in
cardiovascular physiopathology as well as by its emerging role in the
regulation of chemokine receptors. (C) 1998 Federation of European Bio
chemical Societies.