👤 F. Katsuoka

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2
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Also published as: Fumiki Katsuoka
articles
A.W. Greene, J. Baek, O. Ashenberg +1163 more · 2023 · Cells · MDPI · added 2026-04-20
A.W. Greene, J. Baek, O. Ashenberg, A.E. Keating, W.H. Landschulz, P.F. Johnson, S.L. McKnight, C.R. Vinson, K.C. Garcia, J. Lekstrom-Himes, K.G. Xanthopoulos, P. Agre, T. Hai, S.M. Boyd, J.R. Newman, J. Jumper, R. Evans, A. Pritzel, T. Green, M. Figurnov, O. Ronneberger, K. Tunyasuvunakool, R. Bates, A. Zidek, A. Potapenko, M. Varadi, S. Anyango, M. Deshpande, S. Nair, C. Natassia, G. Yordanova, D. Yuan, O. Stroe, G. Wood, A. Laydon, T.K. Sears, J.M. Angelastro, P. Deng, C.M. Haynes, P. Paerhati, J. Liu, Z. Jin, T. Jakos, S. Zhu, L. Qian, J. Zhu, Y. Yuan, T. Sebastian, J.J. Smink, A. Leutz, S.E. van der Krieken, H.E. Popeijus, R.P. Mensink, J. Plat, M. Pulido-Salgado, J.M. Vidal-Taboada, J. Saura, M. Miller, A.J. Spike, J.M. Rosen, K. Balamurugan, E. Sterneck, L. Klimaschewski, S. Tang, O.V. Vitolo, T.A. Weissman, L.T. Donlin, M.L. Shelanski, L.A. Greene, J.M. Aletta, A. Rukenstein, S.H. Green, T.N. Ignatova, V.G. Kukekov, D.A. Steindler, G.B. Stengren, C. Mendelsohn, J.L. Mason, J.E. Goldman, G. Lin, M. Umemura, T. Ogura, A. Matsuzaki, H. Nakano, K. Takao, T. Miyakawa, Y. Takahashi, Y. Kaneko, R. Tanabe, L.R. Devireddy, J.G. Teodoro, F.A. Richard, M.R. Green, S.P. Persengiev, Z. Sheng, L. Li, L.J. Zhu, T.W. Smith, A. Demers, A.H. Ross, R.P. Moser, P.D. Canoll, J. Kuo, M. Weicker, A. Costa, J.N. Bruce, R. Huang, D. Qian, M. Hu, X. Zhang, J. Song, H. Chen, B. Wang, M. Wang, L. Wei, L. Zhang, D.X. Liu, J. Feldheim, A.F. Kessler, D. Schmitt, L. Wilczek, T. Linsenmann, M. Dahlmann, C.M. Monoranu, R.I. Ernestus, C. Hagemann, M. Lohr, D. York, C.D. Sproul, N. Chikere, P.J. Dickinson, T. Wang, R. Yang, J.L. Huang, G. Jiang, Q.X. Song, X. Gu, X.L. Wang, H.H. Song, L.P. Chen, Y.Y. Lin, D. Jiang, D. Zhou, L.R. Palam, L. Jiang, J. Narasimhan, K.A. Staschke, R.C. Wek, M. Costa-Mattioli, P. Walter, X.M. Hua, J. Wang, D.M. Qian, J.Y. Song, X.L. Zhu, R. Zhou, Y.D. Zhao, X.Z. Zhou, Z. Li, H. Li, H. Xie, M. Fan, N. Zhang, J. Ma, S. Che, H.Y. Lee, S.E. Monaco, M. Szabolcs, S. Dong, C.L. Nutt, R.A. Betensky, A.O. Stemmer-Rachamimov, N.C. Denko, K.L. Ligon, D.H. Rowitch, D.N. Louis, X. Wang, F. Xing, I. Herskowitz, B.N. Nguyen, L.W. Elmore, S.E. Holt, S. Dejager, M. Mietus-Snyder, A. Friera, R.E. Pitas, D. Krylov, M. Olive, C. Vinson, S.C. Williams, C. Dezan, D.R. Echlin, K. Gardner, E. Taparowsky, A. Arias, M.W. Lame, L. Santarelli, R. Hen, M. Assanah, R. Lochhead, A. Ogden, J. Bruce, J. Goldman, P. Canoll, G. Hesselager, L. Uhrbom, B. Westermark, M. Nister, N. Vale, D. Duarte, S. Silva, A.S. Correia, B. Costa, M.J. Gouveia, A. Ferreira, E. Dupont, A. Prochiantz, A. Joliot, C.C. Cates, A.D. Arias, L.S. Nakayama Wong, M. Sidorov, G. Cayanan, D.J. Rowland, J. Fung, G. Karpel-Massler, M.D. Siegelin, N.A. Ciaccio, T.S. Reynolds, C.R. Middaugh, J.S. Laurence, B.A. Horst, C. Shu, L. Chau, T. Tsujiuchi, C.S. Peters, X. Liang, S. Li, S. Kannan, Y. Peng, R. Taub, R.H. Diamond, M.L. Moreno, R.L. Bauer, X. Sun, P. Jefferson, Q. Zhou, T. Nakajima, S. Kinoshita, T. Sasagawa, K. Sasaki, M. Naruto, T. Kishimoto, S. Akira, J. Homma, R. Yamanaka, N. Yajima, N. Tsuchiya, N. Genkai, M. Sano, R. Tanaka, M.S. Carro, W.K. Lim, M.J. Alvarez, R.J. Bollo, X. Zhao, E.Y. Snyder, E.P. Sulman, S.L. Anne, F. Doetsch, H. Colman, L.A. Cooper, D.A. Gutman, C. Chisolm, C. Appin, J. Kong, Y. Rong, T. Kurc, E.G. Van Meir, J.H. Saltz, C.S. Moreno, T. Chu, E.J. Rice, G.T. Booth, H.H. Salamanca, Z. Wang, L.J. Core, S.L. Longo, R.J. Corona, L.S. Chin, J.T. Lis, T. Kudo, M.T. Prentzell, S.R. Mohapatra, F. Sahm, Z. Zhao, I. Grummt, W. Wick, C.A. Opitz, M. Platten, E.W. Green, K. Lei, Y. Xia, X.C. Wang, E.H. Ahn, L. Jin, K. Ye, D. Wang, X. Ruan, X. Liu, Y. Xue, L. Shao, C. Yang, L. Zhu, Y. Yang, B. Yu, S.M. Wang, W.C. Lin, H.Y. Lin, Y.L. Chen, C.Y. Ko, J.M. Wang, J. Halliday, K. Helmy, S.S. Pattwell, K.L. Pitter, Q. LaPlant, T. Ozawa, E.C. Holland, M. Minata, A. Audia, J. Shi, S. Lu, J. Bernstock, M.S. Pavlyukov, A. Das, S.H. Kim, Y.J. Shin, Y. Lee, J. Yin, Y.T. Oh, J.Y. Kim, S.S. Kim, E. Choi, T.H. Kim, J.H. Hong, N. Chang, H.J. Cho, J.K. Sa, D. Aguilar-Morante, M. Cortes-Canteli, M. Sanz-Sancristobal, A. Santos, A. Perez-Castillo, J.A. Morales-Garcia, F. Di Pascale, S. Nama, M. Muhuri, S. Quah, H.M. Ismail, X.H.D. Chan, G.M. Sundaram, R. Ramalingam, B. Burke, P. Sampath, T.I. Hsu, J.Y. Chuang, T.J. Kao, S.W. Lim, W.B. Yang, C.C. Huang, Y.T. Tsai, W.C. Chang, K. Biserova, A. Jakovlevs, R. Uljanovs, I. Strumfa, Y. Gao, B. Liu, L. Feng, B. Sun, S. He, G. Wu, G. E, C. Liu, Z. Gao, J. Xu, Y. Fan, Y. Qi, S. Wang, S. Zhao, X. Guo, H. Xue, L. Deng, R. Zhao, L. Selagea, A. Mishra, M. Anand, J. Ross, C. Tucker-Burden, D.J. Brat, X. Kong, W. Meng, Z. Zhou, Y. Li, B. Zhou, R. Wang, L. Zhan, L. Yang, W. Yu, Q. Wu, J. Lian, F. Li, S. Liu, A. Li, Z. He, K. Shao, W. Pu, J. Zhang, S. Guo, F. Qian, I. Glurich, Q. Jin, Y. Ma, S. Ju, Z. Zhang, X. Tang, Y. Liang, G. Sun, Q. He, H. Qu, P. Gao, Y. Shu, H. Bao, S. Han, Z. Liu, N. Zhao, W. Yuan, C. Jian, X. Shu, J. Pang, L. Wang, Q. Dong, D. Jin, I.C. Salaroglio, D.C. Belisario, M. Akman, S. La Vecchia, M. Godel, D.P. Anobile, G. Ortone, S. Digiovanni, S. Fontana, C. Costamagna, K. Okazaki, H. Anzawa, N. Ota, H. Kitamura, Y. Onodera, M.M. Alam, D. Matsumaru, T. Suzuki, F. Katsuoka, K. Kinoshita, H. Sekine, H. Motohashi, M. Liu, R. Li, T. Liu, D. Zhang, M. Shen, X. Ren, Q. Sun, B.A. Sterken, T. Ackermann, C. Muller, H.R. Zuidhof, G. Kortman, A. Hernandez-Segura, M. Broekhuis, D. Spierings, V. Guryev, C.F. Calkhoven, X.Z. Liu, A. Rulina, M.H. Choi, L. Pedersen, J. Lepland, S.T. Takle, N. Madeleine, S.D. Peters, C.E. Wogsland, S.M. Grondal, D. Xia, H. Cao, C. Wu, Z. Sun, H. Liu, L.L. Lee, S.J. Kim, Y.I. Hahn, J.H. Jang, S. Saeidi, Y.J. Surh, H. Wu, J. Gu, W. Cheng, Y. Wang, Q. Wang, R. Zhang, X. Li, H. Zhang, H. Xu, F. Wang, L. Tang, K. Ning, N. Geng, F. Liu, D. Mendoza-Villanueva, S. Sharan, G.H. Summers, L.E. Dobrolecki, M.T. Lewis, J. Cao, S. Ben-Shmuel, R. Rashed, R. Rostoker, E. Isakov, Z. Shen-Orr, D. Leroith, E. Kurzejamska, J. Johansson, K. Jirstrom, V. Prakash, S. Ananthaseshan, L. Boon, J. Fuxe, P. Religa, B.H. Park, S. Kook, S. Lee, J.H. Jeong, A. Brufsky, B.C. Lee, A. Chen, J. Lu, D. Liu, X.X. Zhang, M.C. Li, C.H. Cao, D.Y. Wan, B.X. Xi, J.H. Tan, Z.Y. Yang, X.X. Feng, J. Tan, X. Zheng, M. Li, F. Ye, C. Song, C. Xu, W. Li, S. Zeng, S. Yang, R. Cheng, B. Pang, P. Sun, T.C. Hour, Y.L. Lai, C.I. Kuan, C.K. Chou, H.Y. Tu, H.T. Hu, C.S. Lin, W.J. Wu, Y.S. Pu, B. Jin, Y. Gong, L. Jiao, D. Xin, L. Zhou, Y. Jin, J. Zhou, H. Tian, X. Zhi, Z. Xiao, T. Chen, H. Yuan, Q. Chen, M. Chen, J. Yang, G. Regalo, P. Canedo, G. Suriano, C. Resende, M.L. Campos, M.J. Oliveira, C. Figueiredo, P. Rodrigues-Pereira, N. Blin, R. Seruca, S. Du, Z. Yang, X. Lu, S. Yousuf, M. Zhao, J. Miao, H. Yu, X. Zhu, M.H. Kim, A.Z. Minton, V. Agrawal, D.J. Barakat, J. Mendonca, T. Barberi, S.K. Kachhap, I. Paz-Priel, A.D. Friedman, S.R. Denmeade, D. Li, S. Huang, X. Bi, X. Pu, H. Adamo, P. Hammarsten, C. Hagglof, T. Dahl Scherdin, L. Egevad, P. Stattin, S. Halin Bergstrom, A. Bergh, W.J. Wang, H.Y. Lai, F. Zhang, W.J. Shen, P.Y. Chu, H.Y. Liang, Y.B. Liu, X. Song, C.S. Huang, J. Chu, X.X. Zhu, J.H. Li, X.T. Huang, J.P. Cai, W. Zhao, X.Y. Yin, A. Ramirez, J.L. Jorcano, R.C. Smart, Z.J. Messenger, J.R. Hall, D.D. Jima, J.S. House, H.W. Tam, D.A. Tokarz, Y. Zhou, Q. Xu, B. Yang, S. Jiang, L. Hu, Q. Li, Y. Shuai, E. Fan, Q. Zhong, G. Feng, X. Gou, G. Zhang, Q. Du, Z. Tan, F. Shi, M. Tang, L. Xie, L. Zhao, J. Hu, M. Zhou, A. Bode, Q. Huang, Y. Lv, Y. Dong, D. Song, Y. Shen, Y. Shi, M. Zhang, L. Rong, B. Chen, K. Liu, X. He, J. Li, M. He, F. Yang, L. Chai, Z. Xu, L. Kong, L.J. Cao, Y.J. Zhang, S.Q. Dong, X.Z. Li, X.T. Tong, D. Chen, Z.Y. Wu, X.H. Zheng, W.Q. Xue, W.H. Jia, M. Qin, F. Han, J. Wu, F.X. Gao, D.X. Yan, X.M. He, Y. Long, X.P. Tang, D.L. Ren, F. He, H. Xiao, Y. Cai, A. Swoboda, R. Soukup, O. Eckel, K. Kinslechner, B. Wingelhofer, D. Schorghofer, C. Sternberg, H.T.T. Pham, M. Vallianou, J. Horvath, G. Ambrosini, C. Do, B. Tycko, R.B. Realubit, C. Karan, E. Musi, R.D. Carvajal, V. Chua, A.E. Aplin, G.K. Schwartz, A. Nachiyappan, J.L.J. Soon, H.J. Lim, V.K. Lee, R. Taneja, C. Lai, L.F. Shen, R.R. Zhou, Y.Y. Zhang, P. Rajbhandari, G. Lopez, C. Capdevila, B. Salvatori, J. Yu, R. Rodriguez-Barrueco, D. Martinez, M. Yarmarkovich, N. Weichert-Leahey, B.J. Abraham, Z.Y. Hua, J.N. Hansen, S.K. Dai, Y. Choi, M.D. Fulton, S.M. Lloyd, M. Szemes, J. Sen, H.F. Ding, J.D. Gardiner, L.M. Abegglen, X. Huang, B.E. Carter, E.A. Schackmann, M. Stucki, C.N. Paxton, R. Lor Randall, J.F. Amatruda, A.R. Putnam, Y.H. Wang, H.Y. Huang, W.M. Li, B.W. Yeh, T.F. Wu, Y.L. Shiue, J.J. Sheu, C.F. Li, Y.Y. Chu, C.J. Yen, T.C. Chan, C.H. Hsing, S.K. Huang, K.L. Hsieh, Y.H. Kuo, M.V. Yusenko, A. Trentmann, D.A. Casolari, L. Abdel Ghani, M. Lenz, M. Horn, W. Dorner, S. Klempnauer, H.D. Mootz, M.F. Arteaga, K.H. Klempnauer, D. Frank, R. Moorthy, J.C. Widen, C. Khandanpour, D.A. Harki, J. Rousseau, V. Gagne, M. Labuda, C. Beaubois, D. Sinnett, C. Laverdiere, A. Moghrabi, S.E. Sallan, L.B. Silverman, D. Neuberg, Y.H. Youssef, S.M. Makkeyah, A.F. Soliman, N.H. Meky, M. Kurata, I. Onishi, T. Takahara, Y. Yamazaki, S. Ishibashi, R. Goitsuka, D. Kitamura, J. Takita, Y. Hayashi, D.A. Largaesapda, E. Duprez, A.K. Mittal, G.V. Hegde, P. Aoun, R.G. Bociek, B.J. Dave, A.D. Joshi, W.G. Sanger, D.D. Weisenburger, S.S. Joshi, R. Pal, M. Janz, D.L. Galson, M. Gries, K. Johrens, I. Anagnostopoulos, B. Dorken, M.Y. Mapara, L. Borghesi, R. Piva, E. Pellegrino, M. Mattioli, L. Agnelli, L. Lombardi, F. Boccalatte, G. Costa, B.A. Ruggeri, M. Cheng, R. Chiarle, B. Bisikirska, M. Bansal, J. Teruya-Feldstein, R. Chaganti, A. Califano, J.H. White, R.A. McIllhinney, A. Wise, F. Ciruela, W.Y. Chan, P.C. Emson, A. Billinton, F.H. Marshall, X. Jiang, L. Su, Q. Zhang, C. He, P. Yi, Q. Shu, Y. Tan, J.A. Morris, G. Kandpal, L. Ma, C.P. Austin, C. Kakiuchi, M. Ishiwata, S. Nanko, H. Kunugi, Y. Minabe, K. Nakamura, N. Mori, K. Fujii, K. Yamada, T. Yoshikawa, X. Gao, Y. Mi, N. Guo, Z. Hu, F. Hu, L. Gao, W. Jin, B. Madarampalli, K. Lengel, Y. Xu, G. Li, Z. Lu, C.J. Fiorese, A.M. Schulz, Y.F. Lin, N. Rosin, M.W. Pellegrino, T. Dohi, C.M. Raskett, G.M. Orlowski, C.M. Powers, C.A. Gilbert, J. Plescia, D.C. Altieri, R. Keerthiga, D.S. Pei, A. Fu, Y. Zhao, Y.D. Zhang, S.W. Qian, Z.C. Zhang, S.F. Li, L. Guo, Y. Liu, B. Wen, Q.Y. Lei, A. Khramushin, Z. Ben-Aharon, T. Tsaban, J.K. Varga, O. Avraham, O. Schueler-Furman, N. Pasquier, T.T.T. Nguyen, E. Darvishi, L. Ghamsari, S.F. Leong, R. Ramirez, M. Koester, E. Gallagher, M. Yu, J.M. Mason, G. Merutka, B.J. Kappel, D. Dluzen, D. Tacelosky, M. Moreau, S.P. Wheatley, S.N. Brun, S.L. Markant, L.A. Esparza, G. Garcia, D. Terry, J.M. Huang, X.N. Li, G.A. Grant, J.R. Crawford, R. Frazzi, X. Tong, P. Yang, K. Wang, X. Shan, K. Zhang, D. Merino, D.A. Putavet, P.L.J. de Keizer, L. Bousset, J. Gil, J. Salotti, K. Sakchaisri, W.G. Tourtellotte, L.M. Podust, A.M. Krezel, Y. Kim, H. Tominaga, S. Maeda, M. Hayashi, S. Takeda, S. Komiya, T. Nakamura, H. Akiyama, T. Imamura, I.K. Mann, R. Chatterjee, J. Zhao, M.T. Weirauch, T.R. Hughes, S.M. Ebert, S.A. Bullard, N. Basisty, G.R. Marcotte, Z.P. Skopec, J.M. Dierdorff, A. Al-Zougbi, K.C. Tomcheck, A.D. DeLau, J.A. Rathmacher, I.M.N. Wortel, L.T. van der Meer, M.S. Kilberg, F.N. van Leeuwen, S. Moeckel, K. LaFrance, J. Wetsch, C. Seliger, M.J. Riemenschneider, M. Proescholdt, P. Hau, A. Vollmann-Zwerenz, N.I. Lorenz, A.C.M. Sittig, H. Urban, A.L. Luger, A.L. Engel, C. Munch, J.P. Steinbach, M.W. Ronellenfitsch, C. Chen, P. Liu, S. Fang, Y. You, S. Kaspar, C. Oertlin, K. Szczepanowska, A. Kukat, K. Senft, C. Lucas, S. Brodesser, M. Hatzoglou, O. Larsson, I. Topisirovic, S.E. Parkin, M. Baer, T.D. Copeland, R.C. Schwartz, C.J. Huggins, R. Malik, S. Thomas, N. Martin, O.A. Quinones, W.G. Alvord, M.E. Olanich, J.R. Keller, Z. Renfro, B.E. White, K.E. Stephens, J.M. Adams, S. Cory, C.T. Ishida, Y. Zhang, M.E. Halatsch, M.A. Westhoff, D. Kaloni, S.T. Diepstraten, A. Strasser, G.L. Kelly, M.A. Anderson, P.E. Czabotar, G. Lessene, A.L. Koessinger, C. Cloix, D. Koessinger, D.H. Heiland, F.J. Bock, K. Strathdee, K. Kinch, L. Martinez-Escardo, N.R. Paul, C. Nixon, W. He, M. Morsch, M. Ismail, F.U. Rehman, M. Zheng, R. Chung, M.D. Wendt, S.H.M. Wong, W.Y. Kong, C.M. Fang, H.S. Loh, L.H. Chuah, S. Abdullah, S.C. Ngai, X. Zhai, P. Liang, H. Cui, S. Ishihara, M. Yasuda, A. Ishizu, M. Ishikawa, H. Shirato, H. Haga, S. Banerjee, N. Aykin-Burns, K.J. Krager, S.K. Shah, S.B. Melnyk, M. Hauer-Jensen, S.A. Pawar, D.Y. Zhang, C. Dmello, L. Chen, V.A. Arrieta, E. Gonzalez-Buendia, J.R. Kane, L.P. Magnusson, A. Baran, C.D. James, C. Horbinski, I. Ullah, K. Chung, S. Bae, C. Kim, B. Choi, H.Y. Nam, C.O. Yun, K.Y. Lee, P. Weyerhauser, S.R. Kantelhardt, E.L. Kim, N.J. Caron, S.P. Quenneville, J.P. Tremblay, S.Y. Van Der Zanden, X. Qiao, J. Neefjes, V. Aragon-Sanabria, A. Aditya, F. Chen, B. Yoo, T. Cao, B. Madajewski, R. Lee, M.Z. Turker, K. Ma, F. Iwamoto, V. Gondi, N. Butowski, G. Falchook, A. Williams, K. Peters, J. Evans, N. Lakhani, M. McKean, S. Symeonides, J. Dauparas, I. Anishchenko, N. Bennett, H. Bai, R.J. Ragotte, L.F. Milles, B.I.M. Wicky, A. Courbet, R.J. de Haas, N. Bethel, L. Chang, A. Mondal, A. Perez, R.A. Bottens, T. Yamada, A. Shoari, R. Tooyserkani, M. Tahmasebi, D. Lowik Show less
Developing novel therapeutics often follows three steps: target identification, design of strategies to suppress target activity and drug development to implement the strategies. In this review, we re Show more
Developing novel therapeutics often follows three steps: target identification, design of strategies to suppress target activity and drug development to implement the strategies. In this review, we recount the evidence identifying the basic leucine zipper transcription factors ATF5, CEBPB, and CEBPD as targets for brain and other malignancies. We describe strategies that exploit the structures of the three factors to create inhibitory dominant-negative (DN) mutant forms that selectively suppress growth and survival of cancer cells. We then discuss and compare four peptides (CP-DN-ATF5, Dpep, Bpep and ST101) in which DN sequences are joined with cell-penetrating domains to create drugs that pass through tissue barriers and into cells. The peptide drugs show both efficacy and safety in suppressing growth and in the survival of brain and other cancers in vivo, and ST101 is currently in clinical trials for solid tumors, including GBM. We further consider known mechanisms by which the peptides act and how these have been exploited in rationally designed combination therapies. We additionally discuss lacunae in our knowledge about the peptides that merit further research. Finally, we suggest both short- and long-term directions for creating new generations of drugs targeting ATF5, CEBPB, CEBPD, and other transcription factors for treating brain and other malignancies. Show less
📄 PDF DOI: 10.3390/cells12040581
amino-acid review
Kouhei Tsuchida, Tadayuki Tsujita, Makiko Hayashi +8 more · 2017 · Free radical biology & medicine · Elsevier · added 2026-04-20
The KEAP1-NRF2 system regulates the cellular defence against oxidative and xenobiotic stresses. NRF2 is a transcription factor that activates the expression of cytoprotective genes encoding antioxidat Show more
The KEAP1-NRF2 system regulates the cellular defence against oxidative and xenobiotic stresses. NRF2 is a transcription factor that activates the expression of cytoprotective genes encoding antioxidative, detoxifying and metabolic enzymes as well as transporters. Under normal conditions, KEAP1 represses NRF2 activity by degrading the NRF2 protein. When cells are exposed to stresses, KEAP1 stops promoting NRF2 degradation, and NRF2 rapidly accumulates and activates the transcription of target genes. Constitutive accumulation of NRF2 via a variety of mechanisms that disrupt KEAP1-mediated NRF2 degradation has been observed in various cancer types. Constitutive NRF2 accumulation confers cancer cells with a proliferative advantage as well as resistance to anti-cancer drugs and radiotherapies. To suppress the chemo- and radio-resistance of cancer cells caused by NRF2 accumulation, we conducted high-throughput chemical library screening for NRF2 inhibitors and identified febrifugine derivatives. We found that application of the less-toxic derivative halofuginone in a low dose range rapidly reduced NRF2 protein levels. Halofuginone induced a cellular amino acid starvation response that repressed global protein synthesis and rapidly depleted NRF2. Halofuginone treatment ameliorated the resistance of NRF2-addicted cancer cells to anti-cancer drugs both in vitro and in vivo. These results provide preclinical proof-of-concept evidence for halofuginone as an NRF2 inhibitor applicable to treatment of chemo- and radio-resistant forms of cancer. Show less
no PDF DOI: 10.1016/j.freeradbiomed.2016.12.041
amino-acid synthesis