Identification of cell-active lysine specific demethylase 1-selective inhibitors.

@article{Ueda2009IdentificationOC,
  title={Identification of cell-active lysine specific demethylase 1-selective inhibitors.},
  author={Rie Ueda and Takayoshi Suzuki and Koshiki Mino and Hiroki Tsumoto and Hidehiko Nakagawa and Makoto Hasegawa and Richard M. Sasaki and Tamio Mizukami and Norio Miyata},
  journal={Journal of the American Chemical Society},
  year={2009},
  volume={131 48},
  pages={
          17536-7
        }
}
Lysine specific demethylase 1 (LSD1) plays a key role in the regulation of gene expression by removing the methyl groups from methylated Lys4 of histone H3 (H3K4). Here we report the identification of the first small-molecule LSD1-selective inhibitors. These inhibitors show in vivo H3K4-methylating activity and antiproliferative activity and should be useful as lead structures for anticancer drugs and as tools for studying the biological roles of LSD1. 
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JA907055Q Table 1. In Vitro LSD1-, MAO-A-, and MAO-B-Inhibitory Activities of Compounds 1 and 2 and PCPA IC50 (μM) selectivity cmpd LSD1 MAO-A MAO-B MAO-A/LSD1 MAO-B/LSD1 PCPA

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