Coordinated control of bile acids and lipogenesis through FXR-dependent regulation of fatty acid synthase

J Lipid Res. 2006 Dec;47(12):2754-61. doi: 10.1194/jlr.M600342-JLR200. Epub 2006 Sep 6.

Abstract

We discovered a nuclear receptor element in the FAS promoter consisting of an inverted repeat spaced by one nucleotide (IR-1) and located 21 bases downstream of a direct repeat sequenced by 4 nucleotides (DR-4) oxysterol liver X receptor response element. An IR-1 is present in promoters of several genes of bile acid and lipid homeostasis and binds farnesoid X receptor/retinoid X receptor (FXR/RXR) heterodimers to mediate bile acid-dependent transcription. We show that FXR/RXRalpha specifically binds to the FAS IR-1 and that the FAS promoter is activated approximately 10-fold by the addition of a synthetic FXR agonist in transient transfection assays. We also demonstrate that endogenous FXR binds directly to the murine FAS promoter in the hepatic genome using a tissue-based chromatin immunoprecipitation procedure. Furthermore, we show that feeding wild-type mice a chow diet supplemented with the natural FXR agonist chenodeoxycholic acid results in a significant induction of FAS mRNA expression. Thus, we have identified a novel IR-1 in the FAS promoter and demonstrate that it mediates FXR/bile acid regulation of the FAS gene. These findings provide the first evidence for direct regulation of lipogenesis by bile acids and also provide a mechanistic rationale for previously unexplained observations regarding bile acid control of FAS expression.

Publication types

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

MeSH terms

  • Animals
  • Bile Acids and Salts / metabolism*
  • Binding Sites / genetics
  • Cell Line
  • DNA / genetics
  • DNA / metabolism
  • DNA-Binding Proteins / genetics
  • DNA-Binding Proteins / metabolism*
  • Fatty Acid Synthases / genetics
  • Fatty Acid Synthases / metabolism*
  • Humans
  • Lipogenesis / physiology*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Molecular Sequence Data
  • Promoter Regions, Genetic
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Rats
  • Receptors, Cytoplasmic and Nuclear / genetics
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism
  • Retinoid X Receptor alpha / genetics
  • Retinoid X Receptor alpha / metabolism
  • Sequence Homology, Nucleic Acid
  • Transcription Factors / genetics
  • Transcription Factors / metabolism*
  • Transfection

Substances

  • Bile Acids and Salts
  • DNA-Binding Proteins
  • RNA, Messenger
  • Receptors, Cytoplasmic and Nuclear
  • Recombinant Proteins
  • Retinoid X Receptor alpha
  • Transcription Factors
  • farnesoid X-activated receptor
  • DNA
  • Fatty Acid Synthases