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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.
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
Print publication date: 26/09/2013
Online publication date: 21/08/2013
ISSN (print): 0022-2623
ISSN (electronic): 1520-4804
Publisher: American Chemical Society
PubMed id: 23964788
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