2011 Fiscal Year Final Research Report
Design and synthesis of dual activated bioprobe for proteins and DNAs
| Project/Area Number |
22790009
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Chemical pharmacy
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| Research Institution | Kyoto University |
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Principal Investigator |
TAKASU Kiyosei 京都大学, 大学院・薬学研究科, 教授 (10302168)
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| Project Period (FY) |
2010 – 2011
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| Keywords | ケミカルバイオロジー / 有機合成化学 / 生体高分子 / 化学修飾 / DNA切断活性 / シクロブタン / pH応答 |
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| Research Abstract |
We have developed pH-responsible DNA cleaving agents using fused-cyclobutanols as precursors activated via ring contraction rearrangement. It is important for improvement of reactivity to design molecules stabilizing cation intermediates. In addition, we found that benzo-fused cyclobutanol showed DNA cleavage activity and this activity was stronger with higher concentration and more acidic pH condition. Further investigation about DNA alkylation mechanism and higher active compounds are ongoing in our laboratory.
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