2012 Fiscal Year Final Research Report
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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| Keywords | 医薬分子設計 |
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| 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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