-
J Zhu,
H Wang,
F Chen,
J Fu,
Y Xu,
Y Hou,
HH Kou,
C Zhai,
MB Nelson,
Q Zhang,
ME Andersen,
and
J Pi.
An overview of chemical inhibitors of the Nrf2-ARE signaling pathway and their potential applications in cancer therapy.
Free Radic Biol Med
99
: 544-556
(Oct 12, 2016).
[abstract]
[pubmed]
The Nuclear factor erythroid 2-related factor 2 (Nrf2) is a key transcription factor regulating a wide array of genes for antioxidant and detoxification enzymes in response to oxidative and xenobiotic stress. A large number of Nrf2-antioxidant response element (ARE) activators have been screened for use as chemopreventive agents in oxidative stress-related diseases and even cancer. However, constitutive activation of Nrf2 occurs in a variety of cancers. Aberrant activation of Nrf2 is correlated with cancer progression, chemoresistance, and radioresistance. In this review, we examine recent studies of Nrf2-ARE inhibitors in the context of cancer therapy. We enumerate the possible Nrf2-inhibiting mechanisms of these compounds, their effects sensitizing cancer cells to chemotherapeutic agents, and the prospect of applying them in clinical cancer therapy.
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