Prostacyclin receptor regulation--from transcription to trafficking

Curr Mol Med. 2011 Oct;11(7):517-28. doi: 10.2174/156652411800615144.

Abstract

The prostacyclin receptor (IP--International Union of Pharmacology nomenclature) is a member of the seven transmembrane G-protein coupled receptor (GPCR) superfamily. Recent concerns with selective and non-selective COX-1/COX-2 inhibition have exposed an important cardioprotective role for IP in preventing atherothrombosis. Receptor dysfunction (genetic variants) or reduced signaling (COX-2 inhibition) in high cardiovascular risk patients leads to increased cardiovascular events. These clinical observations have also been confirmed genetically by mouse knockout studies. Thus, receptor regulation is paramount in ensuring correct function in the prevention of atherothrombosis. This review summarizes recent literature on how this important receptor is regulated, from transcription to transport (to and from the membrane surface). These regulatory processes are critical in ensuring that IP receptors are adequately expressed and functional on the cell surface.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Cell Membrane / metabolism*
  • Cyclooxygenase 2 / metabolism
  • Humans
  • Protein Multimerization
  • Protein Transport
  • Receptors, Epoprostenol / genetics*
  • Receptors, Epoprostenol / metabolism*
  • Transcription, Genetic*

Substances

  • Receptors, Epoprostenol
  • Cyclooxygenase 2