2013 Fiscal Year Final Research Report
Discovery of lysine-specific demethylase 1 Inhibitors based on enzymatic mechanism
| Project/Area Number |
24890193
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| Research Category |
Grant-in-Aid for Research Activity Start-up
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | Kyoto Prefectural University of Medicine |
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Principal Investigator |
ITOH Yukihiro 京都府立医科大学, 医学(系)研究科(研究院), 助教 (30636402)
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| Project Period (FY) |
2012-08-31 – 2014-03-31
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| Keywords | 創薬化学 / ドラッグデザイン / 低分子薬物 / エピジェネティクス / ケミカルバイオロジー |
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| Research Abstract |
Selective inhibitors of lysine-specific demethylase 1 (LSD1) are considered to be candidate anticancer agents. Phenylcyclopropylamine (PCPA) is a best-known LSD1 inhibitor, but its potency and selectivity are inadequate. In this study, on the basis of the concept that LSD1 could be potently and selectively inactivated by delivering PCPA directly to the enzyme's active site, LSD1 inhibitors were designed by conjugating PCPA moiety with a lysine moiety as a carrier targeting LSD1. As a result of their synthesis and biological evaluation, LSD1 inhibitors that showed high activity and selectivity were identified.
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[Journal Article] Lysine-Specific Demethylase 1-Selective Inactivators Based on Protein-Targeted Drug Delivery Mechanism2013
Author(s)
Daisuke Ogasawara, Yukihiro Itoh, Hiroki Tsumoto, Taeko Kakizawa, Koshiki Mino, Kiyoshi Fukuhara, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Naoki Miyata, Takayoshi Suzuki
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Journal Title
Angewandte Chemie International Edition
Volume: 52
Pages: 8520-8624
DOI
Peer Reviewed
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