A salt bridge turns off the foot-pocket in class-II HDACs

文献情報

出版日 2016-07-07

DOI 10.1039/C6CP03144G

インパクトファクター 3.676

著者

Jingwei Zhou, Zuolong Yang, Fan Zhang, Hai-Bin Luo, Min Li, Ruibo Wu

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要旨

Histone Deacetylases (HDACs) are promising anticancer targets and several selective inhibitors have been created based on the architectural differences of foot-pockets among HDACs. However, the “gate-keeper” of foot-pockets is still controversial. Herein, it is for the first time revealed that a conserved R–E salt bridge plays a critical role in keeping foot-pockets closed in class-II HDACs by computational simulations. This finding is further substantiated by our mutagenesis experiments.

掲載誌

Physical Chemistry Chemical Physics

CiteScore: 5.5

自己引用率: 10.3%

年間論文数: 3036

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