Synthesis and Activity of Tyropeptin A Derivatives as Potent and Selective Inhibitors of Mammalian 20S Proteasome
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概要
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Tyropeptin A, a potent proteasome inhibitor, was isolated from the culture broth of Kitasatospora sp. MK993-dF2. We synthesized the derivatives of tyropeptin A to enhance its inhibitory potency. Among the synthesized derivatives, the most potent compound, TP-104, exhibited a 20-fold inhibitory potency enhancement for chymotrypsin-like activity of 20S proteasome compared to tyropeptin A. Additionally, TP-110 specifically inhibited the chymotrypsin-like activity, but did not inhibit the post-glutamyl-peptide hydrolyzing (PGPH) and the trypsin-like activities of 20S proteasome. In vitro TP-110 strongly inhibited the growth of various cell lines.
著者
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Hattori S
Microbial Chemistry Research Center
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HIROSAWA Sahei
Institute of Microbial Chemistry
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Imoto M
Department Of Applied Chemistry Faculty Of Science And Technology Keio University
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Ikeda Daishiro
Numazu Bio-medical Research Institute Microbial Chemistry Research Center
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Iijima Masatomi
Numazu Bio-medical Research Institute Microbial Chemistry Research Center
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Iinuma Hironobu
Microbial Chemistry Res. Center
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UMEZAWA Yoji
Microbial Chemistry Research Foundation
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Momose Isao
Numazu Bio-medical Research Institute Microbial Chemistry Research Center
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HIROSAWA Sehei
Hiyoshi Medicinal Chemistry Research Institute, Microbial Chemistry Research Center
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UMEZAWA Yoji
Microbial Chemistry Research Center
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IINUMA Hironobu
Microbial Chemistry Research Center
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