| Project/Area Number |
16K15516
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Infectious disease medicine
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| Research Institution | Nagoya University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
黒崎 博雅 金城学院大学, 薬学部, 教授 (70234599)
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| Co-Investigator(Renkei-kenkyūsha) |
KIMURA Kouji 名古屋大学, 大学院医学系研究科, 准教授 (50425675)
WACHINO Jun-ichi 名古屋大学, 大学院医学系研究科, 講師 (00535651)
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| Research Collaborator |
JIN Wanchun 名古屋大学, 大学院医学系研究科, 特任助教
Kumar Anupuriya 名古屋大学, 大学院医学系研究科, 特任助教
YOKOYAMA Satoru 名古屋大学, 大学院医学系研究科
KANECHI Leo 名古屋大学, 大学院医学系研究科
KANAYAMA Takato 名古屋大学, 大学院医学系研究科
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| Project Period (FY) |
2016-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥3,380,000 (Direct Cost: ¥2,600,000、Indirect Cost: ¥780,000)
Fiscal Year 2016: ¥3,380,000 (Direct Cost: ¥2,600,000、Indirect Cost: ¥780,000)
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| Keywords | カルバペネマーゼ / 既承認薬 / ハイスループット / ニトロセフィン / 阻害剤 / メタロβ-ラクタマーゼ / 阻害薬 |
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| Outline of Final Research Achievements |
Our object is to develop effective inhibitors of carbapenemases, β-lactamases with carbapenem hydrolyzing activity. In this study, we screened for carbapenemase inhibitors among 1018 approved drug compounds. To access this, high-throughput screening technique using purified carbapenemase, nitrocefin, and inhibitor candidate compounds, were developed. This HTS technique made us to evaluate the large number of compounds with ease and reliability in a short time. As a result, we could find 13 weak inhibitors, 11 intermediate inhibitors, and 9 strong inhibitors of one carbapenemase.
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