Identification of Cell-active Lysine Specific Demethylase 1-selective Inhibitors

Overview

Journal J Am Chem Soc

Publisher American Chemical Society

Specialty Chemistry

Date 2009 Dec 3

PMID 19950987

Citations 73

Authors

Rie Ueda

Takayoshi Suzuki

Koshiki Mino

Hiroki Tsumoto

Hidehiko Nakagawa

Makoto Hasegawa

Ryuzo Sasaki

Tamio Mizukami

Naoki Miyata

Affiliations

Soon will be listed here.

Abstract

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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