Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A

Isomers of chiral drugs can exhibit marked differences in biological activities. We studied the binding and inhibitory activities of 12 compounds against KDM5A. Among them are two pairs of enantiomers representing two distinct inhibitor chemotypes, namely, (R)- and (S)-2-((2-chlorophenyl)­(2-(piperi...

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Veröffentlicht in:Journal of medicinal chemistry 2018-04, Vol.61 (7), p.3193-3208
Hauptverfasser: Horton, John R, Liu, Xu, Wu, Lizhen, Zhang, Kai, Shanks, John, Zhang, Xing, Rai, Ganesha, Mott, Bryan T, Jansen, Daniel J, Kales, Stephen C, Henderson, Mark J, Pohida, Katherine, Fang, Yuhong, Hu, Xin, Jadhav, Ajit, Maloney, David J, Hall, Matthew D, Simeonov, Anton, Fu, Haian, Vertino, Paula M, Yan, Qin, Cheng, Xiaodong
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Sprache:eng
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