Design, Synthesis, and Evaluation of 2??(arylsulfonyl) oxiranes as Cell??permeable Covalent Inhibitors of Protein Tyrosine Phosphatases

…, KJ Mark, D Ramai, EJ Chang, TT Talele…

文献索引：Dana, Dibyendu; Das, Tirtha K.; Kumar, Ish; Davalos, Anibal R.; Mark, Kevin J.; Ramai, Daryl; Chang, Emmanuel J.; Talele, Tanaji T.; Kumar, Sanjai Chemical Biology and Drug Design, 2012 , vol. 80, # 4 p. 489 - 499

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被引用次数: 1

摘要

A structure-based design approach has been applied to develop 2-(arylsulfonyl)oxiranes as potential covalent inhibitors of protein tyrosine phosphatases. A detailed kinetic analysis of inactivation by these covalent inhibitors reveals that this class of compounds inhibits a panel of protein tyrosine phosphatases in a time- and dose-dependent manner, consistent with the covalent modification of the enzyme active site. An inactivation experiment in the presence of sodium arsenate, ...