Mechanisms of regulation of G protein-coupled receptor kinases (GRKs) and cardiovascular disease

Cardiovasc Res. 2006 Jan;69(1):46-56. doi: 10.1016/j.cardiores.2005.09.011. Epub 2005 Nov 8.


The G protein-coupled receptor kinases (GRKs) participate with arrestins in the regulation and signal propagation of multiple G protein-coupled receptors (GPCR) of key physiological and pharmacological relevance in the cardiovascular system. The complex mechanisms of regulation of GRK expression, degradation and function are being unveiled gradually. The levels of these kinases are known to change in pathological situations such as heart failure, hypertrophy and hypertension, and in animal models of these diseases. A better understanding of the mechanisms underlying these changes and of how these alterations participate in the triggering or progression of cardiovascular disease may contribute to the design of novel diagnostic and therapeutic strategies.

Publication types

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

MeSH terms

  • Animals
  • Cardiovascular Diseases / enzymology*
  • Cardiovascular Diseases / metabolism
  • Isoenzymes / metabolism*
  • Myocardium / enzymology*
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction / physiology*
  • beta-Adrenergic Receptor Kinases / metabolism*


  • Isoenzymes
  • Receptors, G-Protein-Coupled
  • beta-Adrenergic Receptor Kinases