Regulation of hypoxia-inducible factor 2alpha signaling by the stress-responsive deacetylase sirtuin 1

Science. 2009 Jun 5;324(5932):1289-93. doi: 10.1126/science.1169956.

Abstract

To survive in hostile environments, organisms activate stress-responsive transcriptional regulators that coordinately increase production of protective factors. Hypoxia changes cellular metabolism and thus activates redox-sensitive as well as oxygen-dependent signal transducers. We demonstrate that Sirtuin 1 (Sirt1), a redox-sensing deacetylase, selectively stimulates activity of the transcription factor hypoxia-inducible factor 2 alpha (HIF-2alpha) during hypoxia. The effect of Sirt1 on HIF-2alpha required direct interaction of the proteins and intact deacetylase activity of Sirt1. Select lysine residues in HIF-2alpha that are acetylated during hypoxia confer repression of Sirt1 augmentation by small-molecule inhibitors. In cultured cells and mice, decreasing or increasing Sirt1 activity or levels affected expression of the HIF-2alpha target gene erythropoietin accordingly. Thus, Sirt1 promotes HIF-2 signaling during hypoxia and likely other environmental stresses.

Publication types

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

MeSH terms

  • Acetylation
  • Amino Acid Substitution
  • Animals
  • Basic Helix-Loop-Helix Transcription Factors / chemistry
  • Basic Helix-Loop-Helix Transcription Factors / genetics
  • Basic Helix-Loop-Helix Transcription Factors / metabolism*
  • Cell Hypoxia*
  • Cell Line
  • Cell Line, Tumor
  • Erythropoietin / genetics
  • Gene Expression Regulation
  • Humans
  • Kidney / metabolism
  • Liver / embryology
  • Liver / metabolism
  • Mice
  • Mice, Knockout
  • Mutant Proteins / chemistry
  • Mutant Proteins / metabolism
  • Oxidation-Reduction
  • Signal Transduction*
  • Sirtuin 1
  • Sirtuins / genetics
  • Sirtuins / metabolism*

Substances

  • Basic Helix-Loop-Helix Transcription Factors
  • Mutant Proteins
  • Erythropoietin
  • endothelial PAS domain-containing protein 1
  • SIRT1 protein, human
  • Sirt1 protein, mouse
  • Sirtuin 1
  • Sirtuins