SAR studies for epigenetic research based on natural product synthesis
| Project/Area Number |
22590034
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Chemical pharmacy
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| Research Institution | University of Shizuoka |
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Principal Investigator |
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| Project Period (FY) |
2010 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
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| Budget Amount *help |
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2012: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2011: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2010: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Keywords | 天然物合成 / エピジェネティクス / ヒストンメチル化 / 構造活性相関 / Chaetocin / ジスルフィド結合 / 有機化学 / 天然有機化合物 / chaetocin / ジスルフィド / G9a / 天然物化学 / (+)-chaetocin / ヒストンメチル化酵素 / 類縁体 |
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| Research Abstract |
The disorder of gene expression machinery is involved in various diseases including cancer. We have been focusing on controlling mechanism by selective methylation of histone protein that supports the structure of DNA as a novel target for drug discovery. In this study, we have developed an efficient method for the chemical synthesis of (+)-chaetocin, which is one of the promising inhibitors of histone methylation. This method allowed for the preparation of various analogs. Finally, we have succeeded in creating a novel and potent small molecule inhibitor of histone methyltransferase G9a, which is known to be responsible for cancerous diseases.
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Report
(4 results)
Research Products
(31 results)
