2011 Fiscal Year Final Research Report
Development of anti-HIV agents using chemical genomics based on viral self-regulation mechanism
| Project/Area Number |
22659021
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Single-year Grants |
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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 |
TAMAMURA Hirokazu 東京医科歯科大学, 生体材料工学研究所, 教授 (80217182)
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| Project Period (FY) |
2010 – 2011
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| Keywords | インテグラーゼ阻害剤 / マトリックス蛋白 / CD4ミミック / アンタゴニスト / HIV / CXCR4 |
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| Research Abstract |
Several anti-HIV agents have been developed using forward and reverse chemical gemomics. 1) Helical mimetics and staple peptides of Vpr-fragments were synthesized and found to have potent integrase inhibitory activity. 2) Several matrix fragments with cell membrane penetrating signal having anti-HIV activity were developed. 3) Novel CD4 mimic derivatives having potent anti-HIV activity which cause conformational change of gp120 were found. 4) New CXCR4 antagonists with xylene scaffold were developed.
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