Synthesis and Activity of N-oxalylglycine and Its Derivatives As Jumonji C-domain-containing Histone Lysine Demethylase Inhibitors

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2009 Apr 11

PMID 19359167

Citations 56

Authors

Shohei Hamada

Tae-Dong Kim

Takayoshi Suzuki

Yukihiro Itoh

Hiroki Tsumoto

Hidehiko Nakagawa

Ralf Janknecht

Naoki Miyata

Affiliations

Soon will be listed here.

Abstract

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.

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