Compartmentation of Nrf-2 redox control: regulation of cytoplasmic activation by glutathione and DNA binding by thioredoxin-1

Toxicol Sci. 2004 Nov;82(1):308-17. doi: 10.1093/toxsci/kfh231. Epub 2004 Jul 28.

Abstract

Nrf-2 is a redox-sensitive transcription factor that is activated by an oxidative signal in the cytoplasm but has a critical cysteine that must be reduced to bind to DNA in the nucleus. The glutathione (GSH) and thioredoxin (TRX) systems have overlapping functions in thiol/disulfide redox control in both the cytoplasm and the nucleus, and it is unclear whether these are redundant or have unique functions in control of Nrf-2-dependent signaling. To test whether GSH and Trx-1 have distinct functions in Nrf-2 signaling, we selectively modified GSH by metabolic manipulation and selectively modified Trx-1 expression by transient transfection. Cytoplasmic activation of Nrf-2 was measured by its nuclear translocation and nuclear activity of Nrf-2 was measured by expression of a luciferase reporter construct containing an ARE4 from glutamate cysteine ligase. Results showed that tert-butylhydroquinone (TBHQ), a transcriptional activator that functions through Nrf-2/ARE, promoted Nrf-2 nuclear translocation by a type I (thiylation) redox switch which was regulated by GSH not by Trx-1. In contrast, the ARE reporter was principally controlled by nuclear-targeted Trx-1 and not by GSH. The data show that the GSH and TRX systems have unique, compartmented functions in the control of transcriptional regulation by Nrf-2/ARE.

Publication types

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

MeSH terms

  • Acetylcysteine / pharmacology
  • Binding Sites
  • Buthionine Sulfoximine / pharmacology
  • Cell Nucleus / drug effects
  • Cell Nucleus / metabolism
  • DNA / chemistry
  • DNA / metabolism*
  • DNA-Binding Proteins / biosynthesis*
  • Dose-Response Relationship, Drug
  • Gene Expression Regulation*
  • Glutathione / metabolism*
  • HeLa Cells / drug effects
  • HeLa Cells / metabolism
  • Humans
  • Hydroquinones / pharmacology
  • NF-E2-Related Factor 2
  • Oxidation-Reduction
  • Signal Transduction
  • Thioredoxins / chemistry
  • Thioredoxins / genetics*
  • Thioredoxins / metabolism*
  • Trans-Activators / biosynthesis*
  • Transfection

Substances

  • DNA-Binding Proteins
  • Hydroquinones
  • NF-E2-Related Factor 2
  • NFE2L2 protein, human
  • TXN protein, human
  • Trans-Activators
  • Buthionine Sulfoximine
  • Thioredoxins
  • DNA
  • 2-tert-butylhydroquinone
  • Glutathione
  • Acetylcysteine