Is RGS-2 a new drug development target in cardiovascular disease?

Expert Opin Ther Targets. 2004 Aug;8(4):355-8. doi: 10.1517/14728222.8.4.355.


Hypertension is the most common cardiovascular disease. The regulator of G-protein signalling (RGS) proteins modify the activity of G proteins, and mice deficient in RGS-2 are hypertensive. On vascular smooth muscle, RGS-2 is involved in cross-talk between the nitric oxide (NO)-relaxation pathway and thrombin-contraction pathway. RGS-2 binds to the cGMP-dependent protein kinase I-alpha from the NO relaxation pathway to terminate protease-activated receptor-1 signalling. It has been suggested that RGS-2 is a new drug development target for hypertension. Mice deficient in RGS-2 also have impaired antiviral immunity. It is difficult to envisage how RGS-2 could be targeted to have effects on the cardiovascular system without affecting immunity. Also, it is not clear whether or not targeting RGS-2 will have advantages over targeting receptors. Only an increased understanding of the physiological and pathological role of RGS-2 will help us resolve these issues.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Animals
  • Cardiovascular Diseases / drug therapy*
  • Cardiovascular Diseases / genetics
  • Cardiovascular Diseases / metabolism*
  • Drug Delivery Systems / methods*
  • Drug Delivery Systems / trends*
  • Drug Design*
  • Humans
  • Hypertension / drug therapy*
  • Hypertension / genetics
  • Hypertension / metabolism*
  • Mice
  • Mice, Transgenic
  • RGS Proteins / genetics
  • RGS Proteins / metabolism*


  • RGS Proteins
  • Rgs2 protein, mouse