2. Academic Validation
  3. 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

  • Bioorg Med Chem Lett. 2009 May 15;19(10):2852-5. doi: 10.1016/j.bmcl.2009.03.098.
Shohei Hamada 1,  Tae-Dong Kim,  Takayoshi Suzuki,  Yukihiro Itoh,  Hiroki Tsumoto,  Hidehiko Nakagawa,  Ralf Janknecht,  Naoki Miyata
Affiliations

Affiliation

  • 1 Nagoya City University, Tanabe-dori, Mizuho-ku, Aichi, Japan.
PMID: 19359167 DOI: 10.1016/j.bmcl.2009.03.098
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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