Regulators of G protein signaling: potential drug targets for controlling cardiovascular and immune function

Curr Drug Targets Immune Endocr Metabol Disord. 2004 Jun;4(2):107-18. doi: 10.2174/1568008043339938.


Heterotrimeric G-protein-coupled receptors (GPCRs) mediate a wide variety of organismal functions ranging from vision, olfaction, and gustation to the development and physiology of the cardiovascular, neuronal, and immune system. Naturally they are targets of a large number of therapeutic drugs. The regulators of G protein signaling (RGS) are a family of diverse proteins that regulate the GPCR-mediated signaling pathways principally by acting as GTPase activating proteins (GAPs) for the alpha subunit of the heterotrimeric G-proteins. Certain members of the RGS family contain multiple domains and motifs that mediate interactions with other signaling molecules, thus linking GPCR-dependent and GPCR-independent signaling pathways. Because of their ability to fine-tune vital GPCR-mediated processes and recent findings linking them to brain disorders, retinitis pigmentosa, and cancer RGS proteins have become excellent candidates for new drug discovery. The focus of this review is to discuss the roles of the RGS proteins in the development and normal physiology of cardiovascular and immune system, and to explore their potential as drug targets useful for the treatment of pathological conditions of the cardiovascular and immune systems.

Publication types

  • Review

MeSH terms

  • Animals
  • Cardiovascular Diseases / drug therapy*
  • Cardiovascular Diseases / genetics
  • Cardiovascular Diseases / immunology
  • Cardiovascular Diseases / metabolism*
  • Drug Delivery Systems / methods*
  • GTP-Binding Protein Regulators / genetics
  • GTP-Binding Protein Regulators / immunology
  • GTP-Binding Protein Regulators / metabolism*
  • GTP-Binding Protein Regulators / physiology
  • Humans
  • Immunity / drug effects*
  • Immunity / genetics
  • Signal Transduction / drug effects


  • GTP-Binding Protein Regulators