| Project/Area Number |
23390265
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Infectious disease medicine
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| Research Institution | Kumamoto University |
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Principal Investigator |
MITSUYA Hiroaki 熊本大学, 大学院生命科学研究部, 教授 (20136724)
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| Research Collaborator |
GHOSH Arun K. 米国 Purdue 大学, 医学部, 教授
ARNORLD Eddy 米国 Rutgers 大学, 医学部, 教授
KOVARI Ladislau 米国 Wayne 州立大学, 医学部, 教授
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| Project Period (FY) |
2011-04-01 – 2014-03-31
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| Project Status |
Completed (Fiscal Year 2013)
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| Budget Amount *help |
¥19,370,000 (Direct Cost: ¥14,900,000、Indirect Cost: ¥4,470,000)
Fiscal Year 2013: ¥5,590,000 (Direct Cost: ¥4,300,000、Indirect Cost: ¥1,290,000)
Fiscal Year 2012: ¥5,590,000 (Direct Cost: ¥4,300,000、Indirect Cost: ¥1,290,000)
Fiscal Year 2011: ¥8,190,000 (Direct Cost: ¥6,300,000、Indirect Cost: ¥1,890,000)
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| Keywords | 感染症 / HIV / エイズ / HIV酵素二量体化阻害剤 / 創薬 / HIV感染症治療薬開発 / HIVプロテアーゼ二量体 / 薬剤耐性 |
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| Research Abstract |
In this study period, we designed, synthesized and identified two HIV-1 protease inhibitors (PIs), GRL-1388 and GRL-1398, which contain a tetrahydropyrano-tetrahydrofuran moiety and exert potent activity against multi-drug resistant variants including DRV-resistant HIV-1 strains. We also identified GRL-0519, which contains an oxatricyclic-tetrahydrofuran and exerts potent anti-HIV activity against a wide spectrum of drug-resistant HIV-1s and potent activity to block the dimerization of HIV-1 protease monomers. Additionally, we identified a novel PI, GRL-0739, which contains cyclohexane-bis-THF, and GRL-09510, which persistently exerts potent antiviral activity against various multi-drug resistant clinical isolates and laboratory-generated highly PI-resistant variants.
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