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J Med Chem. 2013 Sep 26;56(18):7222-31. doi: 10.1021/jm400624b. Epub 2013 Sep 5.

Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity.

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1
Graduate School of Medical Science, Kyoto Prefectural University of Medicine , 13 Taishogun Nishitakatsukasa-Cho, Kita-ku, Kyoto 603-8334, Japan.

Abstract

Histone N(ε)-methyl lysine demethylases KDM2/7 have been identified as potential targets for cancer therapies. On the basis of the crystal structure of KDM7B, we designed and prepared a series of hydroxamate analogues bearing an alkyl chain. Enzyme assays revealed that compound 9 potently inhibits KDM2A, KDM7A, and KDM7B, with IC50s of 6.8, 0.2, and 1.2 μM, respectively. While inhibitors of KDM4s did not show any effect on cancer cells tested, the KDM2/7-subfamily inhibitor 9 exerted antiproliferative activity, indicating the potential for KDM2/7 inhibitors as anticancer agents.

PMID:
23964788
PMCID:
PMC3929130
DOI:
10.1021/jm400624b
[Indexed for MEDLINE]
Free PMC Article
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