Retinoic acid receptor-related orphan receptor alpha as a therapeutic target in the treatment of dyslipidemia and atherosclerosis

Drug News Perspect. 2006 Mar;19(2):91-7. doi: 10.1358/dnp.2006.19.2.977445.

Abstract

Retinoic acid receptor-related orphan receptor alpha (RORalpha) is a member of the nuclear receptor family. Recently, cholesterol (derivatives) has been identified as an RORalpha ligand and deorphanized this receptor. RORalpha is expressed in many tissues and is therefore a regulator of multiple biological processes. Studies of staggerer mice and in vitro assays indicate a beneficial modulatory role of RORalpha in the pathogenesis of dyslipidemia, inflammation and atherosclerosis. This paper provides an overview on the role of RORalpha in lipid metabolism and discusses its potential therapeutic option for treating lipid and inflammatory disorders leading to atherosclerosis.

Publication types

  • Review

MeSH terms

  • Animals
  • Atherosclerosis / drug therapy
  • Atherosclerosis / metabolism*
  • Atherosclerosis / pathology
  • Cholesterol / physiology
  • Dyslipidemias / drug therapy
  • Dyslipidemias / metabolism*
  • Energy Metabolism
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • Ligands
  • Lipid Metabolism
  • Mice
  • Muscle, Skeletal / metabolism
  • Muscle, Smooth, Vascular / metabolism
  • Muscle, Smooth, Vascular / pathology
  • Nuclear Receptor Subfamily 1, Group F, Member 1
  • Receptors, Cytoplasmic and Nuclear / drug effects*
  • Trans-Activators / drug effects*

Substances

  • Ligands
  • Nuclear Receptor Subfamily 1, Group F, Member 1
  • Receptors, Cytoplasmic and Nuclear
  • Trans-Activators
  • Cholesterol