Development of pseudo-symmetric inhibitors targeted HIV and HTLVproteases
| Project/Area Number |
23790145
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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
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| Research Institution | Kobe Gakuin University |
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Principal Investigator |
HIDAKA Koushi 神戸学院大学, 薬学部, 講師 (30445960)
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| Project Period (FY) |
2011 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2012: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Fiscal Year 2011: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
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| Keywords | 医薬分子設計 / 分子設計 / 酵素 / 阻害剤 / HIVプロテアーゼ / HTLV-Iプロテアーゼ / 擬似対称型阻害剤 / 成人T細胞白血病 / HTLV-I脊髄症 |
|---|
| Research Abstract |
Application of HIV protease inhibitors developed from substrate amino acid sequence to designing method of pseudo-symmetric inhibitors using “HMC-hydrazide” succeeded in obtaining new and potent inhibitors. We confirmed the position of five bridging water molecules in the complex by X-ray crystallography. We explored substituents at the terminals of the inhibitor to find effective compounds for drug resistant mutant protease. We also obtained potent substrate-based HTLV protease inhibitors, which are promising to apply for the pseudo-symmetric inhibitor design.
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Report
(3 results)
Research Products
(20 results)
