Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors
Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors
复制标题
DOI：
10.1021/ja907055q
复制
发表时间：
2009-12-09
影响因子：
15
通讯作者：
Miyata, Naoki
中科院分区：
文献类型：
--
作者：
Ueda, Rie;Suzuki, Takayoshi;Miyata, Naoki
赖氨酸特异性去甲基化酶1 （Lysine specific demethylase 1, LSD1）通过去除组蛋白H3 （H3K4）的甲基化Lys4在基因表达调控中起关键作用。在这里，我们报告了第一个小分子lsd1选择性抑制剂的鉴定。这些抑制剂在体内表现出h3k4甲基化活性和抗增殖活性，可以作为抗癌药物的先导结构和研究LSD1生物学作用的工具。
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.