Regulation of G protein-coupled receptor signalling: focus on the cardiovascular system and regulator of G protein signalling proteins

Eur J Pharmacol. 2008 May 13;585(2-3):278-91. doi: 10.1016/j.ejphar.2008.02.088. Epub 2008 Mar 15.


G protein-coupled receptors (GPCRs) are involved in many biological processes. Therefore, GPCR function is tightly controlled both at receptor level and at the level of signalling components. Well-known mechanisms by which GPCR function can be regulated comprise desensitization/resensitization processes and GPCR up- and downregulation. GPCR function can also be regulated by several proteins that directly interact with the receptor and thereby modulate receptor activity. An additional mechanism by which receptor signalling is regulated involves an emerging class of proteins, the so-called regulators of G protein signalling (RGS). In this review we will describe some of these control mechanisms in more detail with some specific examples in the cardiovascular system. In addition, we will provide an overview on RGS proteins and the involvement of RGS proteins in cardiovascular function.

Publication types

  • Review

MeSH terms

  • Animals
  • Cardiovascular Physiological Phenomena / drug effects*
  • Cardiovascular System / drug effects
  • Cardiovascular System / metabolism
  • Humans
  • RGS Proteins / biosynthesis
  • RGS Proteins / genetics
  • RGS Proteins / physiology*
  • Receptors, G-Protein-Coupled / biosynthesis
  • Receptors, G-Protein-Coupled / drug effects*
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / physiology*
  • Signal Transduction / drug effects*
  • Signal Transduction / genetics
  • Signal Transduction / physiology*


  • RGS Proteins
  • Receptors, G-Protein-Coupled