G protein-coupled receptor kinase 2 (GRK2): mechanisms of regulation and physiological functions

FEBS Lett. 1998 Jun 23;430(1-2):37-40. doi: 10.1016/s0014-5793(98)00495-5.


G protein-coupled receptor kinase 2 (GRK2) plays a key role in determining the rate and extent of G protein-coupled receptor (GPCR) desensitization and resensitization. Recent data indicate that GRK2 activity, subcellular distribution and expression are tightly regulated. The important physiological function of GRK2 as a modulator of the efficacy of 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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Cyclic AMP-Dependent Protein Kinases / metabolism*
  • Cyclic AMP-Dependent Protein Kinases / physiology
  • G-Protein-Coupled Receptor Kinase 3
  • GTP-Binding Proteins / metabolism*
  • Humans
  • Mice
  • Receptors, Cell Surface / metabolism*
  • Receptors, Cell Surface / physiology
  • Subcellular Fractions
  • beta-Adrenergic Receptor Kinases


  • Receptors, Cell Surface
  • Cyclic AMP-Dependent Protein Kinases
  • G-Protein-Coupled Receptor Kinase 3
  • GRK3 protein, human
  • GRK3 protein, mouse
  • beta-Adrenergic Receptor Kinases
  • GTP-Binding Proteins