| Project/Area Number |
21810015
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| Research Category |
Grant-in-Aid for Research Activity Start-up
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| Allocation Type | Single-year Grants |
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| Research Field |
Living organism molecular science
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| Research Institution | Kyoto University |
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Principal Investigator |
WATANABE Bunta Kyoto University, 化学研究所, 助教 (10544637)
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| Research Collaborator |
HIRATAKE Jun 京都大学, 化学研究所, 教授 (80199075)
HIBI Takao 福井県立大学, 生物資源学部, 教授 (00285181)
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| Project Period (FY) |
2009 – 2010
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| Project Status |
Completed (Fiscal Year 2010)
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| Budget Amount *help |
¥2,756,000 (Direct Cost: ¥2,120,000、Indirect Cost: ¥636,000)
Fiscal Year 2010: ¥1,313,000 (Direct Cost: ¥1,010,000、Indirect Cost: ¥303,000)
Fiscal Year 2009: ¥1,443,000 (Direct Cost: ¥1,110,000、Indirect Cost: ¥333,000)
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| Keywords | 有機科学 / 酵素反応 / グルタチオン / 感染症 / 化学療法剤 / ドラッグデザイン / 有機化学 |
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| Research Abstract |
This research is aimed to develop novel antiinfective drugs using (2S)-2-amino-4-(2-carboxybutylsulfonimidoyl) butyric acid, a potent γ-glutamylcysteine synthetase (γ-GCS) inhibitor, as a precursor. Hydrophobic amino acids were conjugated to N-terminal of the lead compound. The synthetic prodrugs significantly decreased glutathione content of E. coli as compared to the precursor. This result suggested that 1) these prodrugs were uptaken into E.coli and decomposed by peptidases, and 2) the liberated inhibitor inactivated E.coli γ-GCS in situ.
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