Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors

…, J Eckman, J Fan, A Fekete, B Firestone…

文献索引：Shultz, Michael D.; Cao, Xueying; Chen, Christine H.; Cho, Young Shin; Davis, Nicole R.; Eckman, Joe; Fan, Jianmei; Fekete, Alex; Firestone, Brant; Flynn, Julie; Green, Jack; Growney, Joseph D.; Holmqvist, Mats; Hsu, Meier; Jansson, Daniel; Jiang, Lei; Kwon, Paul; Liu, Gang; Lombardo, Franco; Lu, Qiang; Majumdar, Dyuti; Meta, Christopher; Perez, Lawrence; Pu, Minying; Ramsey, Tim; Remiszewski, Stacy; Skolnik, Suzanne; Traebert, Martin; Urban, Laszlo; Uttamsingh, Vinita; Wang, Ping; Whitebread, Steven; Whitehead, Lewis; Yan-Neale, Yan; Yao, Yung-Mae; Zhou, Liping; Atadja, Peter Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4752 - 4772

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被引用次数: 30

摘要

Histone deacetylase (HDAC) inhibitors have shown promise in treating various forms of cancer. However, many HDAC inhibitors from diverse structural classes have been associated with QT prolongation in humans. Inhibition of the human ether a-go-go related gene (hERG) channel has been associated with QT prolongation and fatal arrhythmias. To determine if the observed cardiac effects of HDAC inhibitors in humans is due to hERG ...