2013 Fiscal Year Final Research Report
Structural analysis of HIV integrase multimerization and development of inhibitors of integrase interactions with cellular cofactos
| Project/Area Number |
25670467
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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 |
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科, 教授 (20136724)
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| Project Period (FY) |
2013-04-01 – 2014-03-31
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| Keywords | HIVインテグラーゼ（IN） / IN多量体阻害 / BiFC法 / 新規薬剤の開発 |
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| Research Abstract |
In the present study period, we analyzed the dynamics of IN multimerization and attemoted to elucidate the mechanism of the inhibition of the multimerization by drugs using a newly generated quantitative bimolecular fluorescence complementation (BiFC) assay system. We found that such drugs cause over-multimerization of IN subunits and that EC50 of IN multimerization of the drugs was quite similar to that of their anti-HIV-1 EC50. Continuation of the drug discovery efforts on agents with such unique activity should not only shed lights to the understanding of IN's multimerization mechanism and but also help develop novel HIV treatment strategies for combating multi-drug resistant HIV-1.
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Research Products
(5 results)
