title: Small molecule modulators of antioxidant response pathway.
abstract: 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.
authors.affiliation: Department of Cancer Biology, Dana-Farber Cancer Institute, 250 Longwood Ave, Boston, MA 02115, USA.
authors.forename: Wooyoung
authors.initials: W
authors.lastname: Hur
authors.forename: Nathanael S
authors.initials: NS
authors.lastname: Gray
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D051267:NF-E2-Related Factor 2 / Q000378:metabolism; D015398:Signal Transduction; D054852:Small Molecule Libraries / Q000378:metabolism*; D015533:Transcriptional Activation
chemical_list: D000975:Antioxidants; D051267:NF-E2-Related Factor 2; D054852:Small Molecule Libraries