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

Bioorganic & Medicinal Chemistry Letters, 2009
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.
Shohei, Hamada   +7 more
openaire   +2 more sources

Design, Synthesis, Enzyme-Inhibitory Activity, and Effect on Human Cancer Cells of a Novel Series of Jumonji Domain-Containing Protein 2 Histone Demethylase Inhibitors

Journal of Medicinal Chemistry, 2010
Selective inhibitors of Jumonji domain-containing protein (JMJD) histone demethylases are candidate anticancer agents as well as potential tools for elucidating the biological functions of JMJDs. On the basis of the crystal structure of JMJD2A and a homology model of JMJD2C, we designed and prepared a series of hydroxamate analogues bearing a tertiary ...
Shohei, Hamada   +16 more
openaire   +2 more sources

Nitric Oxide Modifies Histone Methylation Patterns by Inhibiting Jumonji C Domain Containing Demethylases

Free Radical Biology and Medicine, 2012
Jason R. Hickok   +2 more
openaire   +1 more source

High Temperature Triggers Differential Expression of JUMONJI C (JmjC) Domain-Containing Histone Demethylase Genes in Leaf and Stolon Tissues of Potato (Solanum tuberosum L.) Genotypes

Journal of Plant Growth Regulation, 2023
Surbhi Mali   +10 more
openaire   +1 more source

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