Development of Inhibitors for Metallo-beta-lactamases
| Project/Area Number |
15K08458
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Bacteriology (including mycology)
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| Research Institution | Chiba University |
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Principal Investigator |
Hoshino Tyuji 千葉大学, 大学院薬学研究院, 准教授 (90257220)
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2017: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | 阻害化合物 / 薬剤耐性菌 / メタロβ-ラクタマーゼ / 理論薬物設計 / 有機合成 / X線結晶構造解析 / 酵素活性阻害 / 構造活性相関 |
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| Outline of Final Research Achievements |
Beta-lactamase is one kind of enzymes which dissociate beta-lactam antibiotics such as penicillin and imipenem. Many bacteria that are resistant to antibiotics carry the genome of beta-lactamase and generate it for drug-resistance. In this study, we focused on the metallo-beta-lactamase that is high enzymatic activity among several types of beta-lactamases. As a consequence of the in silico and in vitro chemical screening, we identified three chemical compounds that block the action of metallo-beta-lactamase. Two of them were synthesized in our study and utilized as a fundamental skeleton of further chemical modification. The other one was purchased from a supplier. We successfully obtained the binding structure between metallo-beta-lactamase and one of the identified compounds. The information of the binding structure will be important for the rational design of the chemicals that have high inhibitory potency.
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Report
(4 results)
Research Products
(18 results)
