2014 Fiscal Year Final Research Report
The activating mechanism of the FGFR3 pathogenic mutants
| Project/Area Number |
24590056
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Physical pharmacy
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| Research Institution | Osaka Prefecture University |
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Principal Investigator |
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Keywords | 受容体型キナーゼ / 病原活性変異体 / Ｘ線結晶構造解析 / 酵素機能解析 / ＦＧＦＲ３ |
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| Outline of Final Research Achievements |
In order to facilitate drug discovery for cancer, we aim to elucidate the activating mechanism of the FGFR3 pathogenic mutants by the functional and crystallographic analyses. The Km (ATP) values of N540T, K650M, and G697C mutants varied from 0.30- to 108-hold compared with that of the wild type. The result implies that these mutants are activated via distinguished mechanisms. The exploration of crystallization condition has yielded the micro-crystals of the wild type and mutants. Ongoingly, we will perform the crystal analyses and elucidate the molecular mechanisms for the activation of the active mutants.
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| Free Research Field |
シグナル伝達蛋白質の構造機能解析および創薬化学研究
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