Discovery of novel Myc-Max heterodimer disruptors with a three-dimensional pharmacophore model.
Discovery of novel Myc-Max heterodimer disruptors with a three-dimensional pharmacophore model.
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DOI：
10.1021/jm801278g
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发表时间：
2009-03-12
影响因子：
7.3
通讯作者：
Bahar I
中科院分区：
文献类型：
--
作者：
Mustata G;Follis AV;Hammoudeh DI;Metallo SJ;Wang H;Prochownik EV;Lazo JS;Bahar I
A 3-dimensional pharmacophore model was generated utilizing a set of known inhibitors of c-Myc-Max heterodimer formation. The model successfully identified a set of structurally diverse compounds with potential inhibitory activity against c-Myc. Nine compounds were tested in vitro, and four displayed affinities in the µM range and growth inhibitory activity against c-Myc-overexpressing cells. These studies demonstrate the applicability of pharmacophore modeling to the identification of novel and potentially more puissant inhibitors of the c-Myc oncoprotein.
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