2010 Fiscal Year Final Research Report
Molecular design and synthesis of soluble NF-κB inhibitor and suppression of ovarian carcinoma
| Project/Area Number |
20611015
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Chemical biology
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| Research Institution | Keio University |
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Principal Investigator |
UMEZAWA Kazuo Keio University, 理工学部, 教授 (70114402)
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| Co-Investigator(Kenkyū-buntansha) |
SUGAI Takeshi 慶應義塾大学, 薬学部, 教授 (60171120)
BANNO Kouji 慶應義塾大学, 医学部, 講師 (70265875)
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| Project Period (FY) |
2008 – 2010
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| Keywords | DHMEQ / NF-κB / 卵巣癌 / 分子デザイン / 腹腔内播種 / 浸潤 / 転移 / 抗癌剤 |
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| Research Abstract |
Our newly found NF-κB inhibitor DHMEQ is very specific and ameliorates many disease models in animal experiments. However, it is hardly soluble to most solvents. Then, we have prepared more soluble DHMEQ analogs. We found that DHMEQ inhibited cellular invasion of ovarian carcinoma cells. As the new mechanism of inhibition, inhibition of the CXCL12/CXCR4 system with downstream proteases was suggested to be involved. In addition, DHMEQ increased the sensitivity of ovarian carcinoma cells to anticancer agents, and suppressed cachexia in ovarian cancer-bearing mice,.
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[Journal Article] Chemoenzymatic synthesis of (2S,3S,4S)-form2010
Author(s)
M. Hamada, Y. Niitsu, C. Hiraoka, I. Kozawa, T. Higashi, M. Shoji, K. Umezawa, T. Sugai
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Journal Title
the physiologically active stereoisomer of dehydroxymethylepoxyquinomicin (DHMEQ), a potent inhibitor on NF-κB. Tetrahedron 66
Pages: 7083-7087
Peer Reviewed
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