An attempt to develop novel CaM kinase phosphatase inhibitors that are effective for suppression of cancer metastasis with low cytotoxicity
| Project/Area Number |
15K01824
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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 |
Chemical biology
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| Research Institution | Hiroshima University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
根平 達夫 広島大学, 総合科学研究科, 准教授 (60321692)
石原 康宏 広島大学, 総合科学研究科, 助教 (80435073)
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| Research Collaborator |
HIDE Michihiro 広島大学, 大学院・医歯薬保健学研究科, 教授 (50284188)
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2017: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2016: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2015: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Keywords | プロテインホスファターゼ / 阻害剤 / スクリーニング / がん転移・浸潤 / 細胞遊走 / 細胞毒性 / 構造機能相関 / 特異的阻害剤 / 乳がん細胞 / 遊走 / 膜透過性 / ホスファターゼ / タンパク質カルボニル化 / 反応機構 / 特異性 / 活性化因子 / プロトカドヘリン / 浸潤 |
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| Outline of Final Research Achievements |
CaM kinase phosphatase (CaMKP/PPM1F/POPX2) is a Ser/Thr protein phosphatase that belongs to PPM family. Accumulating evidence shows possible involvement of CaMKP in cancer metastasis. In this study, we carried out large-scale screening of chemical library to find CaMKP-specific inhibitors, and investigated a mechanism of action of the inhibition. Subsequently, we showed that some of these inhibitors effectively suppressed migration of breast cancer cells despite the fact that they had no significant toxic effects on the cells. These data suggest that these CaMKP inhibitors or the derivatives are promising lead compounds for the development of novel cancer metastasis inhibitors without significant cytotoxicity.
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Report
(4 results)
Research Products
(19 results)
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[Presentation] Protein conformational analysis by fluorescence-detected circular dichroism (FDCD)2015
Author(s)
Tatsuo Nehira, Kaoru Ishihara, Hirone Ito, Keiko Masuda, Kazuyoshi Ukena, Koichi Matsuo, Shunsuke Izumi, Takeshi Yamazaki, and Atsuhiko Ishida
Organizer
The International Chemical Congress of Pacific Basin Societies 2015
Place of Presentation
Honolulu, Hawaii, USA
Year and Date
2015-12-14
Related Report
Int'l Joint Research
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