Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB.
作者： Matthew B. Soellner , Katherine A. Rawls , Christoph Grundner , Tom Alber , Jonathan A. Ellman
DOI: 10.1021/JA0727520
关键词: Mycobacterium tuberculosis 、 Protein tyrosine phosphatase 、 Phosphatase 、 Substrate (chemistry) 、 Chemistry 、 Tuberculosis 、 Biochemistry 、 Screening method
摘要: A new substrate-based fragment approach for the identification of novel PTP inhibitors is presented. This method was applied to Mycobacterium tuberculosis PtpB, a promising target treatment tuberculosis. resulted in development most potent PtpB inhibitor reported date (0.22 μM) with low molecular weight and good selectivity against panel other protein tyrosine phosphatases.
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