title: Identification of cell-active lysine specific demethylase 1-selective inhibitors.
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.
authors: Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
authors: Rie
authors: R
authors: Ueda
authors: Takayoshi
authors: T
authors: Suzuki
authors: Koshiki
authors: K
authors: Mino
authors: Hiroki
authors: H
authors: Tsumoto
authors: Hidehiko
authors: H
authors: Nakagawa
authors: Makoto
authors: M
authors: Hasegawa
authors: Ryuzo
authors: R
authors: Sasaki
authors: Tamio
authors: T
authors: Mizukami
authors: Naoki
authors: N
authors: Miyata
mesh_terms: D020134:Catalytic Domain; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D056466:Histone Demethylases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D006657:Histones / Q000378:metabolism; D006801:Humans; D008958:Models, Molecular; D013379:Substrate Specificity
chemical_list: D004791:Enzyme Inhibitors; D006657:Histones; D056466:Histone Demethylases; C495195:KDM1A protein, human