| 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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| 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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