Synthesis and activity of N

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• 作者：Shohei Hamada ; Tae-Dong Kim ; Takayoshi Suzuki ; Yukihiro Itoh ; Hiroki Tsumoto ; Hidehiko Nakagawa ; Ralf Janknecht ; Naoki Miyata
• 关键词：Histone lysine demethylase ; N-Oxalylglycine ; Inhibitor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：15 May 2009
• 年：2009
• 卷：19
• 期：10
• 页码：2852-2855
• 全文大小：592 K

文摘

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.