| Project/Area Number |
15K15312
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Cardiovascular medicine
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| Research Institution | Jichi Medical University |
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Principal Investigator |
Nagai Ryozo 自治医科大学, 医学部, 学長 (60207975)
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| Co-Investigator(Kenkyū-buntansha) |
YOKOYAMA Shigeyuki 理化学研究所, 横山構造生物学研究室, 上席研究員 (00159229)
AIZAWA Kenichi 自治医科大学, 医学部, 准教授 (70436484)
NAKAYA Takeo 自治医科大学, 医学部, 講師 (80512277)
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| Project Period (FY) |
2015-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2015: ¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
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| Keywords | PDK4 / 心不全 / 癌 / 立体構造解析 / in silico解析 |
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| Outline of Final Research Achievements |
It is important to improve the PDK4 inhibitors on the basis of X-ray crystallographic analyses of the PDK4 inhibitors bound to the PDK4 protein. We successfully prepared, by the cell-free protein synthesis method, a large amount of the PDK4 protein sample suitable for crystallization. We developed a novel method to form a PDK4 protein covalently bonded with an inhibitor by introducing an unnatural amino acid designed for click chemistry in a specified position of the PDK4 protein. Furthermore, using a heart failure model mouse, we showed that two kinds of new PDK4 inhibitors were useful for the treatment of heart failure.
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