The nuclear receptor Rev-erbalpha is a liver X receptor (LXR) target gene driving a negative feedback loop on select LXR-induced pathways in human macrophages

Mol Endocrinol. 2008 Aug;22(8):1797-811. doi: 10.1210/me.2007-0439. Epub 2008 May 29.

Abstract

A role of the nuclear receptor Rev-erbalpha in the regulation of transcription pathways involving other nuclear receptors is emerging. Indeed, Rev-erbalpha is a negative regulator of transcription by binding to overlapping response elements shared with various nuclear receptors, including the peroxisome proliferator-activated receptors and the retinoid-related orphan receptor alpha (RORalpha). Here, we show that Rev-erbalpha is expressed in primary human macrophages and that its expression is induced by synthetic ligands for the liver X receptors (LXRs), which control cholesterol homeostasis, inflammation, and the immune response in macrophages. LXRalpha binds to a specific response element in the human Rev-erbalpha promoter, thus inducing Rev-erbalpha transcriptional expression. Interestingly, Rev-erbalpha does not influence basal or LXR-regulated cholesterol homeostasis. However, Rev-erbalpha overexpression represses the induction of toll-like receptor (TLR)-4 by LXR agonists, whereas Rev-erbalpha silencing by short interfering RNA results in enhanced TLR-4 expression upon LXR activation. Electrophoretic mobility shift, chromatin immunoprecipitation, and transient transfection experiments demonstrate that Rev-erbalpha represses human TLR-4 promoter activity by binding as a monomer to a RevRE site overlapping with the LXR response element site in the TLR-4 promoter. These data identify Rev-erbalpha as a new LXR target gene, inhibiting LXR-induction of TLR-4 in a negative transcriptional feedback loop, but not cholesterol homeostasis gene expression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Base Sequence
  • Cells, Cultured
  • Cholesterol / metabolism
  • DNA-Binding Proteins / genetics*
  • DNA-Binding Proteins / metabolism*
  • Dimerization
  • Feedback, Physiological* / drug effects
  • Humans
  • Lipopolysaccharides / pharmacology
  • Liver X Receptors
  • Macrophage Activation / drug effects
  • Macrophages / drug effects
  • Macrophages / metabolism*
  • Models, Genetic
  • Molecular Sequence Data
  • Nuclear Receptor Subfamily 1, Group D, Member 1
  • Orphan Nuclear Receptors
  • Protein Binding / drug effects
  • Receptors, Cytoplasmic and Nuclear / genetics*
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Repressor Proteins / metabolism
  • Response Elements / genetics
  • Retinoid X Receptor alpha / metabolism
  • Toll-Like Receptor 4 / genetics
  • Transcriptional Activation / drug effects
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • DNA-Binding Proteins
  • Lipopolysaccharides
  • Liver X Receptors
  • NR1D1 protein, human
  • NR1H3 protein, human
  • Nuclear Receptor Subfamily 1, Group D, Member 1
  • Orphan Nuclear Receptors
  • Receptors, Cytoplasmic and Nuclear
  • Repressor Proteins
  • Retinoid X Receptor alpha
  • TLR4 protein, human
  • Toll-Like Receptor 4
  • Tumor Necrosis Factor-alpha
  • Cholesterol