Small molecule modulators of antioxidant response pathway

Curr Opin Chem Biol. 2011 Feb;15(1):162-73. doi: 10.1016/j.cbpa.2010.12.009. Epub 2010 Dec 30.


Nuclear factor E2-related factor 2 (Nrf2) is a transcription factor that regulates Antioxidant Response Element (ARE)-mediated transcription of a plethora of antioxidant and protective genes to counteract the harmful effects of reactive oxygen species or environmental carcinogens. Studies have demonstrated that pre-emptive activation of the Nrf2-ARE pathway reinforces the cellular defense mechanism against oxidative stress and leads to protection in a variety of disease models. Non-carcinogenic ARE inducers have been identified from a variety of chemical classes that enhance the transcriptional activity of Nrf2 through S-alkylation of reactive cysteines within the cellular redox sensor protein Keap1 (Kelch-like ECH associated protein 1). Here we review the currently known small molecule ARE inducers and their reported biological activities in various models.

Publication types

  • Review

MeSH terms

  • Animals
  • Antioxidants / chemistry
  • Antioxidants / metabolism*
  • Humans
  • NF-E2-Related Factor 2 / metabolism
  • Signal Transduction*
  • Small Molecule Libraries / metabolism*
  • Transcriptional Activation


  • Antioxidants
  • NF-E2-Related Factor 2
  • Small Molecule Libraries