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

…, Y Itoh, H Tsumoto, H Nakagawa, R Janknecht…

文献索引：Hamada, Shohei; Kim, Tae-Dong; Suzuki, Takayoshi; Itoh, Yukihiro; Tsumoto, Hiroki; Nakagawa, Hidehiko; Janknecht, Ralf; Miyata, Naoki Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 10 p. 2852 - 2855

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被引用次数: 77

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.