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

页码：17536 / 17537

页数：2