Two stress-responsive kinases suppress ferroptosis by activating antioxidant programs under mild oxidative stress

Cancer cells maintain chronically elevated levels of reactive oxygen species (ROS) while relying on robust antioxidant programs to preserve redox homeostasis and viability. Although therapeutic strategies that disrupt this balance to induce lethal oxidative stress and ferroptosis have emerged as promising anticancer approaches, the upstream signaling mechanisms that constrain ROS accumulation under physiologically relevant stress conditions remain incompletely understood. Here, we identify the stress-responsive kinases SMG1 and DNA-dependent protein kinase (DNA-PK) as functionally redundant regulators of redox homeostasis and ferroptosis resistance. Genetic or pharmacological inhibition of either kinase triggers ferroptotic cell death, accompanied by marked accumulation of total ROS, ferrous iron, and lipid hydroperoxides. Mechanistically, under mild oxidative stress, SMG1 and DNA-PK cooperatively phosphorylate the central antioxidant transcription factor NRF2 at serine 13 and serine 40, weakening its interaction with the negative regulator KEAP1 and promoting NRF2 accumulation and transcriptional activation. Transcriptomic profiling of de novo mRNAs revealed that inhibition of either kinase is sufficient to suppress NRF2-driven antioxidant gene expression. In contrast, excessive oxidative stress overrides this pro-survival pathway and redirects signaling toward anti-survival responses mediated by ATF4, ATM-CHK2, and JNK/p38 pathways. Collectively, these findings uncover a previously unrecognized SMG1/DNA-PK-NRF2 signaling axis that functions as a redox stress-intensity-dependent switch governing cell fate decisions between antioxidant adaptation and ferroptotic death. Targeting this axis may represent a promising therapeutic strategy for cancer treatment.

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Journal
Signal Transduction and Targeted Therapy
Published
2026-08-03
DOI
https://doi.org/10.1038/s41392-026-02892-1
Primary Topic
Ferroptosis and cancer prognosis
Type
article
Field-Weighted Citation Impact
0.00

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article

Two stress-responsive kinases suppress ferroptosis by activating antioxidant programs under mild oxidative stress

Akiko Uchiyama, Hiroyuki Satofuka, Minoru Yoshida, Noritaka Kagaya et al.
Signal Transduction and Targeted Therapy
Ferroptosis and cancer prognosis
article

Two stress-responsive kinases suppress ferroptosis by activating antioxidant programs under mild oxidative stress

Akiko Uchiyama, Hiroyuki Satofuka, Minoru Yoshida, Noritaka Kagaya, Hiroyuki Osada, Yukinari Kato, Shigeo Ohno, Takashi Nakayama, Hidehito Kuroyanagi, Hirotatsu Imai, Kae Suzuki, Hiroko Hirose, Kouji Hoshino, Hirotsugu Uemura, Hitomi Kurosawa, Kazuhiko Matsuo, Daisuke Utsumi, Kyoko Aoyagi, Marco A. De Velasco, Hiroji Uemura, Kazuo Shin-ya, Hidehisa Takahashi, Tetsuo Onuki, Mariko Mizuguchi, Yoshie Nakamura, Akio Yamashita, Yumiko Fujikawa, Kenzo Takahashi
article en

Abstract

Cancer cells maintain chronically elevated levels of reactive oxygen species (ROS) while relying on robust antioxidant programs to preserve redox homeostasis and viability. Although therapeutic strategies that disrupt this balance to induce lethal oxidative stress and ferroptosis have emerged as promising anticancer approaches, the upstream signaling mechanisms that constrain ROS accumulation under physiologically relevant stress conditions remain incompletely understood. Here, we identify the stress-responsive kinases SMG1 and DNA-dependent protein kinase (DNA-PK) as functionally redundant regulators of redox homeostasis and ferroptosis resistance. Genetic or pharmacological inhibition of either kinase triggers ferroptotic cell death, accompanied by marked accumulation of total ROS, ferrous iron, and lipid hydroperoxides. Mechanistically, under mild oxidative stress, SMG1 and DNA-PK cooperatively phosphorylate the central antioxidant transcription factor NRF2 at serine 13 and serine 40, weakening its interaction with the negative regulator KEAP1 and promoting NRF2 accumulation and transcriptional activation. Transcriptomic profiling of de novo mRNAs revealed that inhibition of either kinase is sufficient to suppress NRF2-driven antioxidant gene expression. In contrast, excessive oxidative stress overrides this pro-survival pathway and redirects signaling toward anti-survival responses mediated by ATF4, ATM-CHK2, and JNK/p38 pathways. Collectively, these findings uncover a previously unrecognized SMG1/DNA-PK-NRF2 signaling axis that functions as a redox stress-intensity-dependent switch governing cell fate decisions between antioxidant adaptation and ferroptotic death. Targeting this axis may represent a promising therapeutic strategy for cancer treatment.

Signal Transduction and Targeted TherapyVol. 11(1)
Bunkyo University (JP), Tohoku University (JP), Yokohama City University Medical Center (JP), University of the Ryukyus (JP), Juntendo University (JP), RIKEN Center for Sustainable Resource Science (JP), RIKEN (JP), Microbial Chemistry Research Foundation (JP), Kindai University Sakai Hospital (JP), Next Generation Technology (United States) (US), Azabu University (JP), National Institute of Advanced Industrial Science and Technology (JP), The University of Tokyo (JP), Yokohama City University (JP), Kindai University (JP)
Bristol-Myers Squibb, Japan Agency for Medical Research and Development, Kindai University, Kanazawa University, University of Queensland, Japan Society for the Promotion of Science, Japan Science and Technology Agency, RIKEN, National Cancer Institute, Moonshot Research and Development Program, Daiichi Sankyo Europe
Good health and well-being
Openalex Percentile: Top 10%
Ferroptosis and cancer prognosis
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