Brusatol provokes a rapid and transient inhibition of Nrf2 signaling and sensitizes mammalian cells to chemical toxicity—implications for therapeutic targeting of Nrf2

@inproceedings{Olayanju2015BrusatolPA,
  title={Brusatol provokes a rapid and transient inhibition of Nrf2 signaling and sensitizes mammalian cells to chemical toxicity—implications for therapeutic targeting of Nrf2},
  author={Adedamola Olayanju and Ian M Copple and Holly K. Bryan and George T. Edge and Rowena L C Sison and Min Wei Wong and Zheng-Quan Lai and Zhi-Xiu Lin and Karen A. Dunn and Christopher M. Sanderson and Ahmad F. Alghanem and Michael J Cross and Ewa C S Ellis and Magnus Ingelman-Sundberg and Hassan Malik and Neil R. Kitteringham and Christopher E. P. Goldring and Brian Kevin Park},
  booktitle={Free radical biology & medicine},
  year={2015}
}
The transcription factor Nrf2 regulates the basal and inducible expression of a battery of cytoprotective genes. Whereas numerous Nrf2-inducing small molecules have been reported, very few chemical inhibitors of Nrf2 have been identified to date. The quassinoid brusatol has recently been shown to inhibit Nrf2 and ameliorate chemoresistance in vitro and in vivo. Here, we show that brusatol provokes a rapid and transient depletion of Nrf2 protein, through a posttranscriptional mechanism, in mouse… CONTINUE READING
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References

Publications referenced by this paper.
SHOWING 1-10 OF 27 REFERENCES

Nrf2: control of sensitivity to carcinogens

  • Archives of Toxicology
  • 2011
VIEW 5 EXCERPTS
HIGHLY INFLUENTIAL

Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism.

  • Proceedings of the National Academy of Sciences of the United States of America
  • 2011
VIEW 4 EXCERPTS
HIGHLY INFLUENTIAL

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