1454255-89-0Relevant articles and documents
Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity
Suzuki, Takayoshi,Ozasa, Hiroki,Itoh, Yukihiro,Zhan, Peng,Sawada, Hideyuki,Mino, Koshiki,Walport, Louise,Ohkubo, Rei,Kawamura, Akane,Yonezawa, Masato,Tsukada, Yuichi,Tumber, Anthony,Nakagawa, Hidehiko,Hasegawa, Makoto,Sasaki, Ryuzo,Mizukami, Tamio,Schofield, Christopher J.,Miyata, Naoki
, p. 7222 - 7231 (2013/10/21)
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.
