- 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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- KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
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Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDMIA, and methods of increasing gamma globin gene expression in a human or animal subject are also provided for the treatment diseases such as sickle cell disease.
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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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p. 8620 - 8624
(2013/09/12)
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