| Project/Area Number |
16K07710
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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 |
Bioorganic chemistry
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| Research Institution | University of Tsukuba |
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Principal Investigator |
Usui Takeo 筑波大学, 生命環境系, 教授 (60281648)
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| Research Collaborator |
Hayakawa Ichiro
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| Project Period (FY) |
2016-04-01 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2018: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2016: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Keywords | γ-tubulin / 構造活性相関 / 相乗効果 / がん分子標的 / 生理活性物質 / がん分子標的治療 |
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| Outline of Final Research Achievements |
For efficient microtubule polymerization in cells, the γ-tubulin complex, which mainly localizes in the centrosome, is required. However, γ-tubulin functions other than microtubule polymerization remain to be revealed. Also, γ-tubulin is considered as a novel target molecule for cancer chemotherapy, but its target validity remains unknown. In this study, based on the γ-tubulin-specific inhibitor gatastatin we developed ahead of the world, we succeeded in developing a more active γ-tubulin inhibitor and found some known compounds that exhibits synergic activity with gatastatin. These results would provide basic knowledge to clarify the novel intracellular function of γ-tubulin.
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| Academic Significance and Societal Importance of the Research Achievements |
γ-tubulinはがん化学療法の新規標的分子として考えられているが、その妥当性は不明のままである。我々はgatastatinをリード化合物として、より活性の強いγ-tubulin阻害剤の開発に成功するとともに、相乗効果を示す薬剤を見出すことでγ-tubulinの細胞内機能の一端を明らかにすることに成功した。以上の結果は、今後のがん化学療法においてγ-tubulinを標的とする場合の基礎的知見を与えるとともに、γ-tubulinの新規機能を明らかにするための手掛かりとなる情報を提供している。
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