- LSD1-SELECTIVE INHIBITOR HAVING LYSINE STRUCTURE
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A primary object of the present invention is to provide a novel compound having LSD1-selective inhibitory activity and having an antitumor/anticancer action, an antiviral action, and the like. As means for achieving such object, provided is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: [in the formula, R1 to R5, A, and *1 to *3 are as defined in Description].
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Paragraph 0188; 0223, 0229
(2015/11/18)
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- Lysine-specific demethylase 1-selective inactivators: Protein-targeted drug delivery mechanism
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Drug drop off: Given that lysine-specific demethylase 1 (LSD1) could be potently and selectively inactivated by delivering phenylcyclopropylamine (PCPA), a weak and nonselective LSD1 inhibitor, directly to the enzyme's active site, a novel series of LSD1 inactivators (1) were designed. Biological and mechanistic studies indicate that 1 inhibits LSD1 potently and selectively. Copyright
- Ogasawara, Daisuke,Itoh, Yukihiro,Tsumoto, Hiroki,Kakizawa, Taeko,Mino, Koshiki,Fukuhara, Kiyoshi,Nakagawa, Hidehiko,Hasegawa, Makoto,Sasaki, Ryuzo,Mizukami, Tamio,Miyata, Naoki,Suzuki, Takayoshi
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supporting information
p. 8620 - 8624
(2013/09/12)
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