Development of orally active proteasome inhibitors using in vivo imaging.
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 |
Section | 一般 |
Research Field |
Living organism molecular science
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Research Institution | Microbial Chemistry Research Foundation |
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 |
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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Report
(5 results)
Research Products
(30 results)
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[Journal Article] Quinofuracins A-E, produced by the fungus Staphylotrichum boninense PF1444, show p53-dependent growth suppression.2015
Author(s)
Tatsuda D, Momose I, Someno T, Sawa R, Kubota Y, Iijima M, Kunisada T, Watanabe T, Shibasaki M, Nomoto A.
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Journal Title
J. Nat. Prod.
Volume: 78
Issue: 2
Pages: 188-195
DOI
Related Report
Peer Reviewed / Open Access
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[Journal Article] Decalpenic acid induces early osteoblastic markers in pluripotent mesenchymal cells via activation of retinoic acid receptor gamma.2012
Author(s)
Sakamoto, S., Kojima, F., Momose, I., Kawada, M., Adachi, H., and Nishimura, Y.
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Journal Title
Biochem. Biophys. Res. Commun.
Volume: 422
Issue: 4
Pages: 751-757
DOI
Related Report
Peer Reviewed
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[Presentation] Decalpenic acid, a novel small molecule from Penicillium verruculosum CR37010, induces early osteoblastic markers in pluripotent mesenchymal cells through activation of retinoic acid receptor signaling pathway.2011
Author(s)
Shuichi Sakamoto, Fukiko Kojima, Masayuki Igarashi, Ryuichi Sawa, Maya Umekita, Yumiko Kubota, Isao Momose, Koichi Nakae, Hayamitsu Adachi, Yoshio Nishimura, Yuzuru Akamatsu
Organizer
8th AFMC International Medicinal Chemistry Symposium
Place of Presentation
京王プラザホテル東京、東京
Related Report
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