Halofuginone enhances the chemo-sensitivity of cancer cells by suppressing NRF2 accumulation

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• 作者：Kouhei Tsuchida^a ; ¹ ; Tadayuki Tsujita^a ; ^b ; ¹ ; Makiko Hayashi^a ; Asaka Ojima^a ; Nadine Keleku-Lukwete^a ; Fumiki Katsuoka^c ; Akihito Otsuki^d ; Haruhisa Kikuchi^e ; Yoshiteru Oshima^e ; Mikiko Suzuki^f ; ^{suzukimikiko@med.tohoku.ac.jp} ; Masayuki Yamamoto^a ; ^c ; ^{masiyamamoto@med.tohoku.ac.jp}
• 关键词：NRF2 ; Inhibitor ; Cancer ; Halofuginone ; KEAP1
• 刊名：Free Radical Biology and Medicine
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：103
• 期：Complete
• 页码：236-247
• 全文大小：2407 K
• 卷排序：103

文摘

High-throughput screening identified febrifugine derivatives as NRF2 inhibitors. The febrifugine derivative halofuginone (HF) suppresses NRF2 protein accumulation. HF represses protein synthesis via an amino acid starvation response. HF enhances the sensitivity of NRF2-addicted cancer cells to anti-cancer drugs. HF serves as a chemo-sensitizer of NRF2-addicted cancer cells.