Discovery and Structure-Based Optimization of Novel Atg4B Inhibitors for the Treatment of Castration-Resistant Prostate Cancer
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- Yudai Kudo
- Laboratory of Biochemistry, Gifu Pharmaceutical University, Gifu 501-1196, Japan
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- Satoshi Endo
- Laboratory of Biochemistry, Gifu Pharmaceutical University, Gifu 501-1196, Japan
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- Mei Fujita
- Laboratory of Biochemistry, Gifu Pharmaceutical University, Gifu 501-1196, Japan
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- Atsumi Ota
- Laboratory of Biochemistry, Gifu Pharmaceutical University, Gifu 501-1196, Japan
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- Yuji O. Kamatari
- Institute for Glyco-core Research (iGCORE), Gifu University, Gifu 501-1193, Japan
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- Yoshimasa Tanaka
- Center for Medical Innovation, Nagasaki University, 1-7-1 Sakamoto, Nagasaki 852-8588, Japan
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- Takeshi Ishikawa
- Graduate School of Science and Engineering, Kagoshima University, 1-21-40 Korimoto, Kagoshima 890-0065, Japan
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- Hayato Ikeda
- Graduate School of Innovative Life Science, University of Toyama, Toyama 930-8555, Japan
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- Takuya Okada
- Graduate School of Innovative Life Science, University of Toyama, Toyama 930-8555, Japan
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- Naoki Toyooka
- Graduate School of Innovative Life Science, University of Toyama, Toyama 930-8555, Japan
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- Naohiro Fujimoto
- Department of Urology, University of Occupational and Environmental Health, Kitakyushu 807-8555, Japan
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- Toshiyuki Matsunaga
- Education Center of Green Pharmaceutical Sciences, Gifu Pharmaceutical University, Gifu 502-8585, Japan
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- Akira Ikari
- Laboratory of Biochemistry, Gifu Pharmaceutical University, Gifu 501-1196, Japan
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説明
Autophagy inhibition is an attractive target for cancer therapy. In this study, we discovered inhibitors of Atg4B essential for autophagosome formation and evaluated their potential as therapeutics for prostate cancer. Seventeen compounds were identified as candidates after
収録刊行物
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- Journal of Medicinal Chemistry
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Journal of Medicinal Chemistry 65 (6), 4878-4892, 2022-03-04
American Chemical Society (ACS)