| Project/Area Number |
23659059
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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 |
Drug development chemistry
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| Research Institution | Tokyo University of Pharmacy and Life Science |
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Principal Investigator |
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| Project Period (FY) |
2011 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
|
| Budget Amount *help |
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2012: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2011: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | 医薬品化学 / 創薬化学 / プロテアーゼ阻害剤 / 重症急性呼吸器症候群 / ビオチニル化試薬 / 感染症 / 固相合成化学 / システインプロテアーゼ |
|---|
| Research Abstract |
This work describes the establishment of common method for the development of cysteine protease inhibitors based on the aryl-ketone structure. As an example, from our preliminary inhibitor with a mild activity, we developed potent tri- and di-peptide-type SARS-CoV 3CL protease inhibitors. The results suggested that our aryl-ketone strategy worked effectively in the development of viral cysteine protease inhibitors. In addition, we developed a solid phase reagent that can introduce biotin to the target molecules by a very simple procedure in order to obtain a high affinity substrate, which can be changeable to the potent inhibitor by introducing the aryl-ketone structure.
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