A novel Nrf2 pathway inhibitor sensitizes KEAP1-mutant lung cancer cells to chemotherapy
Molecular Cancer Therapeutics — Zhang D, Hou Z, Aldrich KE, et al. | June 24, 2021
A promising target for cancer therapy is Nrf2-Keap1-ARE pathway (a master regulator of oxidative stress), and mutations in NFE2L2, KEAP1, and related genes have been identified in many human malignancies, especially lung cancer, researchers discovered MSU38225, which is a novel small molecule capable of suppressing Nrf2 pathway activity. It was found that not only downregulation of Nrf2 transcriptional activity but also reduction in the expression of Nrf2 downstream targets (including NQO1, GCLC, GCLM, AKR1C2 and UGT1A6) was brought about by MSU38225. In both 2D cell culture and soft agar, inhibition of the growth of human lung cancer cells was caused by MSU38225. It was revealed that MSU38225 sensitized human lung cancer cells to chemotherapies both in vitro and in vivo. Findings indicate that MSU38225, a novel Nrf2 pathway inhibitor, could potentially afford an adjuvant therapy to enhance the response to chemotherapies in patients suffering from lung cancer.
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