2011 Fiscal Year Final Research Report
Development of anti-HIV agents targeting dynamic supramolecular mechanism and feedback mechanism
| Project/Area Number |
21390029
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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 |
Drug development chemistry
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| Research Institution | Tokyo Medical and Dental University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
NOMURA Wataru 東京医科歯科大学, 生体材料工学研究所, 講師 (80463909)
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| Project Period (FY) |
2009 – 2011
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| Keywords | HIV / CXCR4 / CD4ミミック / アンタゴニスト / インテグラーゼ阻害剤 / マトリックス蛋白 |
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| Research Abstract |
In the development of drugs for treatments of HIV infectious disease and AIDS, we have synthesized HIV entry inhibitors having dynamic supramolecular mechanism such CXCR4 antagonists and other novel agents having different action mechanism. 1. Novel CXCR4 antagonists having xylene scaffold and potent bivalent CXCR4 antagonists were developed. 2. Small CD4 mimic derivatives having significant inhibitory activity against HIV entry and causing an increase of binding affinity for neutralizing antibodies were found. 3. Integrase inhibitors were discovered from Vpr fragments. 4. Anti-HIV agents derived from matrix fragments with cell membrane penetrating signals were developed.
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Research Products
(45 results)
