Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors

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• 作者：Rie Ueda ; Takayoshi Suzuki ; Koshiki Mino ; Hiroki Tsumoto ; Hidehiko Nakagawa ; Makoto Hasegawa ; Ryuzo Sasaki ; Tamio Mizukami ; Naoki Miyata
• 刊名：Journal of the American Chemical Society
• 出版年：2009
• 出版时间：December 9, 2009
• 年：2009
• 卷：131
• 期：48
• 页码：17536-17537
• 全文大小：141K
• 年卷期：v.131,no.48(December 9, 2009)
• ISSN：1520-5126

文摘

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.