At Long Last Potent and Selective KDM5 Inhibitors

作者:Rotili Dante*; Mattevi Andrea*
来源:Cell Chemical Biology, 2016, 23(7): 749-751.
DOI:10.1016/j.chembiol.2016.07.003

摘要

Histone lysine demethylase 5 enzymes (KDM5s) have recently been proposed as crucial oncogenic drivers. In this issue of Cell Chemical Biology, Horton et al. (2016) describe results of an extensive structural analysis that reveals how distinct inhibitor chemotypes bind KDM5 and suggest avenues for improving KDM5 inhibitory potency and selectivity.

  • 出版日期2016-7-21