Synthesis of HDAC inhibitors that locally develop their inhibition activity in cells
| Project/Area Number |
24659050
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Nagoya City University |
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Principal Investigator |
MIYATA Naoki 名古屋市立大学, 薬学研究科(研究院), 教授 (50114674)
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| Co-Investigator(Renkei-kenkyūsha) |
NAKAGAWA Hidehiko 名古屋市立大学, 大学院薬学研究科, 教授 (80281674)
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| Research Collaborator |
YAMADA Souta
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2014: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2013: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2012: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
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| Keywords | ヒストン脱アセチル化酵素 / エピジェネティクス / ケミカルバイオロジー / 細胞内局在性 / 光解除性保護基 / 分子標的治療薬 / 制がん剤 / 蛍光検出 / ｴﾋﾟｼﾞｪﾈﾃｨｸｽ / ケージド化合物 / ヒストン脱アセチル化酵素阻害薬 |
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| Outline of Final Research Achievements |
To elucidate the association between the localization and the function of histone deacetylases (HDACs) in cells, we designed and synthesized HDAC inhibitors which locally develop their activity in cells. We used a caged technique to control the HDAC activity. The synthesized HDAC inhibitors with photo-labile protecting group time-dependently inhibited HDAC activity under the visible light irradiation conditions. These results showed that these HDAC inhibitors can be controlled their activity by visible light irradiation even in the living cell systems and become a useful tool to elucidate the association between the localization and the function of HDAC in cells.
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Report
(4 results)
Research Products
(21 results)
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[Journal Article] Design, Synthesis, and Biological Activity of NCC149 Derivatives as Histone Deacetylase 8-Selective Inhibitors.2014
Author(s)
Suzuki T, Muto N, Bando M, Itoh Y, Masaki A, Ri M, Ota Y, Nakagawa H, Iida S, Shirahige K, Miyata N.
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Journal Title
ChemMedChem.
Volume: 9
Issue: 3
Pages: 657-664
DOI
Related Report
Peer Reviewed
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[Journal Article] Rapid Discovery of Highly Potent and Selective Inhibitors of Histone Deacetylase 8 Using Click Chemistry to Generate Candidate Libraries2012
Author(s)
Takayoshi Suzuki, Yosuke Ota, Masaki Ri, Masashige Bando, Aogu Gotoh, Yukihiro Itoh, Hiroki Tsumoto, Prima R. Tatum, Tamio Mizukami, Hidehiko Nakagawa, Shinsuke Iida, Ryuzo Ueda, Katsuhiko Shirahige, and Naoki Miyata.
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Journal Title
J. Med. Chem.
Volume: 55
Issue: 22
Pages: 9562-9575
DOI
Related Report
Peer Reviewed
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[Journal Article] Design, Synthesis, and Biological Activity of a Novel Series of Human Sirtuin-2-Selective Inhibitors2012
Author(s)
Takayoshi Suzuki, Mohammed Naseer Ahmed Khan, Hideyuki Sawada, Erika Imai, Yukihiro Itoh, Katsura Yamatsuta, Natsuko Tokuda, Jun Takeuchi, Takuya Seko, Hidehiko Nakagawa, and Naoki Miyata
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Journal Title
J. Med. Chem.
Volume: 55
Issue: 12
Pages: 5760-5773
DOI
Related Report
Peer Reviewed
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