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

被引：160
|
作者：
Ueda, Rie [1 ]
Suzuki, Takayoshi [1 ]
Mino, Koshiki [2 ]
Tsumoto, Hiroki [1 ]
Nakagawa, Hidehiko [1 ]
Hasegawa, Makoto [2 ]
Sasaki, Ryuzo [3 ]
Mizukami, Tamio [2 ]
Miyata, Naoki [1 ]
机构：
[1] Nagoya City Univ, Grad Sch Pharmaceut Sci, Mizuho Ku, Aichi 4678603, Japan
[2] Nagahama Inst Biosci Technol, Grad Sch Biosci, Shiga 5260829, Japan
[3] Frontier Pharma Inc, Shiga 5260829, Japan
来源：
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2009年 / 131卷 / 48期
基金：
日本学术振兴会;
关键词：
HISTONE DEMETHYLATION; LSD1; RESOLUTION;
D O I：
10.1021/ja907055q
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
(Chemical Equation Presented) 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. © 2009 American Chemical Society.
引用
收藏
页码：17536 / 17537
页数：2
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