Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors

被引：102

作者：

Hamada, Shohei ^{[1
]}

Kim, Tae-Dong ^{[2
]}

Suzuki, Takayoshi ^{[1
]}

Itoh, Yukihiro ^{[1
]}

Tsumoto, Hiroki ^{[1
]}

Nakagawa, Hidehiko ^{[1
]}

Janknecht, Ralf ^{[2
]}

Miyata, Naoki ^{[1
]}

机构：

[1] Nagoya City Univ, Grad Sch Pharmaceut Sci, Mizuho Ku, Aichi 4678603, Japan

[2] Univ Oklahoma, Hlth Sci Ctr, Dept Cell Biol, Oklahoma City, OK 73104 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 10期

基金：

日本学术振兴会;

关键词：

Histone lysine demethylase; N-Oxalylglycine; Inhibitor; TRANSCRIPTION FACTOR ER81; PROTEIN; COACTIVATORS; METHYLATION; ACTIVATION; REPRESSION; RECEPTOR; ENZYMES; JMJD2A; P300;

D O I：

10.1016/j.bmcl.2009.03.098

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-Oxalylglycine (NOG) derivatives were synthesized, and their inhibitory effect on histone lysine demethylase activity was evaluated. NOG and compound 1 inhibited histone lysine demethylases JMJD2A, 2C and 2D in enzyme assays, and their dimethyl ester prodrugs DMOG and 21 exerted histone lysine methylating activity in cellular assays. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2852 / 2855

页数：4

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