Cholestenoic acid is a naturally occurring ligand for liver X receptor alpha

Endocrinology. 2000 Nov;141(11):4180-4. doi: 10.1210/endo.141.11.7772.

Abstract

Excessive cholesterol is eliminated from extrahepatic cells by reverse cholesterol transport, a process by which neutral sterols are transferred to extracellular acceptor lipoproteins for further transport to the liver. Another process independent of lipoproteins involves excretion of 3beta-hydroxy-5-cholesten-25(R)-26-carboxylic (cholestenoic) acid, a metabolite of 27-hydroxycholesterol. Physiological concentrations of cholestenoic acid activated the nuclear receptor liver X receptor alpha (LXR alpha; NR1H3), but not other oxysterol receptors. As a ligand, cholestenoic acid modulated interaction of LXR alpha with the nuclear receptor coactivator Grip-1. Cholestenoic acid, therefore, may function as a signaling molecule for regulation of lipid metabolism via LXR alpha.

Publication types

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

MeSH terms

  • Cell Line
  • Cell Nucleus / metabolism
  • Cholesterol / analogs & derivatives*
  • Cholesterol / metabolism*
  • Cholesterol / pharmacology
  • DNA-Binding Proteins
  • Embryo, Mammalian
  • Genes, Reporter
  • Glutathione Transferase / genetics
  • Humans
  • Kidney
  • Ligands
  • Lipid Metabolism
  • Liver X Receptors
  • Luciferases / genetics
  • Nuclear Receptor Coactivator 2
  • Orphan Nuclear Receptors
  • Receptors, Cytoplasmic and Nuclear*
  • Receptors, Retinoic Acid / drug effects
  • Receptors, Retinoic Acid / genetics
  • Receptors, Retinoic Acid / metabolism*
  • Receptors, Thyroid Hormone / drug effects
  • Receptors, Thyroid Hormone / genetics
  • Receptors, Thyroid Hormone / metabolism*
  • Recombinant Fusion Proteins / metabolism
  • Signal Transduction
  • Transcription Factors / metabolism
  • Transcriptional Activation

Substances

  • DNA-Binding Proteins
  • Ligands
  • Liver X Receptors
  • NCOA2 protein, human
  • NR1H3 protein, human
  • Nuclear Receptor Coactivator 2
  • Orphan Nuclear Receptors
  • Receptors, Cytoplasmic and Nuclear
  • Receptors, Retinoic Acid
  • Receptors, Thyroid Hormone
  • Recombinant Fusion Proteins
  • Transcription Factors
  • 3-hydroxy-5-cholestenoic acid
  • Cholesterol
  • Luciferases
  • Glutathione Transferase