| Project/Area Number |
17K17958
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
Applied pharmacology
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| Research Institution | Kumamoto University |
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Principal Investigator |
Ohura Kayoko 熊本大学, 大学教育統括管理運営機構, 特任助教 (80452879)
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| Project Period (FY) |
2017-04-01 – 2020-03-31
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| Project Status |
Completed (Fiscal Year 2019)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2019: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2018: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2017: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Keywords | 変形性膝関節症 / 血漿加水分解酵素 / 加水分解酵素 / 薬学 / 酵素 |
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| Outline of Final Research Achievements |
In the present study, a quantitative western blotting method was established using fluorophosphonate-biotin, a universal probe of serinesterases, to investigate the characteristics of esterases present in the knee joint. In addition, it was found that the anticholinergic soft drug, 2R3’R-SGM, was mainly hydrolyzed by plasma paraoxonase 1 in the human. Furthermore, the effect of calcium ion on the hydrolysis of cationic and anionic substrate by human butyrylcholinesterase was clarified.
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| Academic Significance and Societal Importance of the Research Achievements |
本研究にて構築したセリンエステラーゼの定量方法は、関節内に存在する加水分解酵素だけでなく、その他の組織に存在する新たな加水分解酵素の同定にも応用可能と期待される。また、これまでに詳細な検討のなかったParaoxonase 1やButyrylcholinesteraseの血漿加水分解酵素の基質認識性および特性を本研究では一部、明らかにすることができ、今後、血漿加水分解酵素を利用したプロドラッグおよびソフトドラッグを設計する上で有用な情報になるものと確信できる。
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