4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 10, Pages 2852-2855

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.03.098

Keywords

Histone lysine demethylase; N-Oxalylglycine; Inhibitor

Funding

  1. Japan Society for the Promotion of Science

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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.

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