| Project/Area Number |
23510270
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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 |
Living organism molecular science
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| Research Institution | Microbial Chemistry Research Foundation |
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Principal Investigator |
MOMOSE Isao 公益財団法人微生物化学研究会, 微生物化学研究所・沼津支所, 主席研究員 (10270547)
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| Co-Investigator(Renkei-kenkyūsha) |
MASUDA Toru 公益財団法人微生物化学研究会, 微生物化学研究所沼津支所, 主席研究員 (90165720)
WATANABE Takumi 公益財団法人微生物化学研究会, 微生物化学研究所, 主席研究員 (80270544)
TATSUDA Daisuke 公益財団法人微生物化学研究会, 微生物化学研究所沼津支所, 研究員 (20442569)
OHBA Shun-ichi 公益財団法人微生物化学研究会, 微生物化学研究所沼津支所, 研究員 (00601600)
ABE Hikaru 公益財団法人微生物化学研究会, 微生物化学研究所, 研究員 (10462269)
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| Project Period (FY) |
2011-04-28 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2014: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2013: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2012: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2011: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | インビボイメージング / プロテアソーム / プロテアソーム阻害剤 / 経口剤 / 経口投与 |
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| Outline of Final Research Achievements |
Proteasome inhibitors were approved for treatment of multiple myeloma. Because these inhibitors are administered by intravenous bolus, new orally active proteasome inhibitors are desired. In this study, we developed a system for in vivo imaging of proteasome inhibition in the tumors of living mice, using a proteasome-sensitive fluorescent reporter. Then we used tyropeptin, which are produced by Kitasatospora sp. MK993-dF2, as a lead compound for the design of proteasome inhibitors, and synthesized tyropeptin derivatives. Finally, we found new orally active proteasome inhibitors using our in vivo imaging system and tyropeptin derivatives.
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