Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors
Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors
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DOI：
10.1016/j.bmcl.2009.03.098
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发表时间：
2009-05-15
影响因子：
2.7
通讯作者：
Miyata, Naoki
中科院分区：
文献类型：
--
作者：
Hamada, Shohei;Kim, Tae-Dong;Miyata, Naoki
合成了N-草酰甘氨酸（NOG）衍生物，并评价了其对组蛋白赖氨酸脱甲基酶活性的抑制作用。NOG和化合物1在酶测定中抑制组蛋白赖氨酸脱甲基酶JMJD 2A、2C和2D，并且它们的二甲酯前体药物DMOG和21在细胞测定中发挥组蛋白赖氨酸甲基化活性。(C)2009爱思唯尔有限公司保留所有权利。
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.