Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB
Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB
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DOI：
10.1021/ja0727520
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发表时间：
2007-08-08
影响因子：
15
通讯作者：
Ellman, Jonathan A.
中科院分区：
文献类型：
--
作者：
Soellner, Matthew B.;Rawls, Katherine A.;Ellman, Jonathan A.
提出了一种新的基于底物的片段鉴定新PTP抑制剂的方法。该方法被应用于结核分枝杆菌PtpB，一个有前途的新的目标，用于治疗结核病。这导致了迄今为止报道的最有效的PtpB抑制剂（0.22 μ M）的开发，其具有低分子量和对一组其他蛋白酪氨酸磷酸酶的良好选择性。
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 new target for the treatment of tuberculosis. This resulted in the development of the most potent PtpB inhibitor reported to date (0.22 mu M) with low molecular weight and good selectivity against a panel of other protein tyrosine phosphatases.