15-hydroxyeicosatetraenoic acid is a preferential peroxisome proliferator-activated receptor beta/delta agonist

Mol Pharmacol. 2010 Feb;77(2):171-84. doi: 10.1124/mol.109.060541. Epub 2009 Nov 10.

Abstract

Peroxisome proliferator-activated receptor (PPARs) modulate target gene expression in response to unsaturated fatty acid ligands, such as arachidonic acid (AA). Here, we report that the AA metabolite 15-hydroxyeicosatetraenoic acid (15-HETE) activates the ligand-dependent activation domain (AF2) of PPARbeta/delta in vivo, competes with synthetic agonists in a PPARbeta/delta ligand binding assay in vitro, and triggers the interaction of PPARbeta/delta with coactivator peptides. These agonistic effects were also seen with PPARalpha and PPARgamma, but to a significantly weaker extent. We further show that 15-HETE strongly induces the expression of the bona fide PPAR target gene Angptl4 in a PPARbeta/delta-dependent manner and, conversely, that inhibition of 15-HETE synthesis reduces PPARbeta/delta transcriptional activity. Consistent with its function as an agonistic ligand, 15-HETE triggers profound changes in chromatin-associated PPARbeta/delta complexes in vivo, including the recruitment of the coactivator cAMP response element-binding protein binding protein. Both 15R-HETE and 15S-HETE are similarly potent at inducing PPARbeta/delta coactivator binding and transcriptional activation, indicating that 15-HETE enantiomers generated by different pathways function as PPARbeta/delta agonists.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Fibroblasts / chemistry
  • Fibroblasts / metabolism
  • Humans
  • Hydroxyeicosatetraenoic Acids / biosynthesis
  • Hydroxyeicosatetraenoic Acids / metabolism
  • Hydroxyeicosatetraenoic Acids / pharmacology*
  • Mice
  • Mice, Knockout
  • Molecular Sequence Data
  • NIH 3T3 Cells
  • PPAR delta / agonists*
  • PPAR delta / genetics
  • PPAR delta / physiology
  • PPAR-beta / agonists*
  • PPAR-beta / genetics
  • PPAR-beta / physiology
  • Trans-Activators / biosynthesis
  • Trans-Activators / genetics
  • Trans-Activators / physiology

Substances

  • Hydroxyeicosatetraenoic Acids
  • PPAR delta
  • PPAR-beta
  • Trans-Activators
  • 15-hydroxy-5,8,11,13-eicosatetraenoic acid