2010 Fiscal Year Self-evaluation Report
Development of drug candidates that epigenetically regulate gene expression
| Project/Area Number |
20390034
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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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 Nagoya City University, 大学院・薬学研究科, 教授 (50114674)
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| Project Period (FY) |
2008 – 2011
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| Keywords | エピジェネティクス / 遺伝子発現制御 / 創薬分子設計 / ヒストン脱メチル化酵素阻害剤 |
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| Research Abstract |
遺伝子発現の制御にかかわる酵素(ヒストン脱メチル化酵素(HDME)、ヒストン脱アセチル化酵素(HDAC)など)をターゲットとし、酵素の構造と作用機序に基づいてアイソザイム選択的阻害化合物を分子設計・合成し、非細胞系および細胞系での活性評価試験を行い、遺伝子発現を制御する医薬品候補化合物を見出す。
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[Journal Article] Design, Synthesis, Enzyme-inhibitory Activity, and Effect on Human Cancer Cells of a Novel Series of Jumonji Domain-Containing Protein 2 Histone Demethylase Inhibitors2010
Author(s)
Shohei Hamada, Takayoshi Suzuki, Koshiki Mino, Koichi Koseki, Felix Oehme, Ingo Flamme, Hiroki Ozasa, Yukihiro Itoh, Daisuke Ogasawara, Haruka Komaarashi, Aiko Katoh, Hiroki Tsumoto, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Naoki Miyata
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Journal Title
J.Med.Chem. 53
Pages: 5629-5638
Peer Reviewed
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[Journal Article] Design, Synthesis, and Biological Activity of Boronic acid-Based Histone Deacetylase Inhibitors2009
Author(s)
Nobuaki Suzuki, Takayoshi Suzuki, Yosuke Ota, Tatsuya Nakano, Masaaki Kurihara, Haruhiro Okuda, Takao Yamori, Hiroki Tsumoto, Hidehiko Nakagawa, Naoki Miyata
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Journal Title
J.Med.Chem. 52
Pages: 2909-2922
Peer Reviewed
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