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

Lookup NU author(s): Professor Akane Kawamura


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Histone Nε-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. © 2013 American Chemical Society.

Publication metadata

Author(s): Suzuki T, Ozasa H, Itoh Y, Zhan P, Sawada H, Mino K, Walport L, Ohkubo R, Kawamura A, Yonezawa M, Tsukada Y, Tumber A, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Schofield CJ, Miyata N

Publication type: Article

Publication status: Published

Journal: Journal of Medicinal Chemistry

Year: 2013

Volume: 56

Issue: 18

Pages: 7222-7231

Print publication date: 26/09/2013

Online publication date: 21/08/2013

ISSN (print): 0022-2623

ISSN (electronic): 1520-4804

Publisher: American Chemical Society


DOI: 10.1021/jm400624b

PubMed id: 23964788


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