Development of molecular probes for second-site screening and design of protein tyrosine phosphatase inhibitors.
Development of molecular probes for second-site screening and design of protein tyrosine phosphatase inhibitors.
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DOI：
10.1021/jm061481l
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发表时间：
2007-05
影响因子：
7.3
通讯作者：
J. Vázquez;L. Tautz;Jennifer J Ryan;K. Vuori;T. Mustelin;M. Pellecchia
中科院分区：
文献类型：
--
作者：
J. Vázquez;L. Tautz;Jennifer J Ryan;K. Vuori;T. Mustelin;M. Pellecchia
We report on the design, synthesis, and evaluation of a series of furanyl-salicyl-nitroxide derivatives as effective chemical probes for second-site screening against phosphotyrosine phosphatases (PTPs) using NMR-based techniques. The compounds have been tested against a panel of PTPs to assess their ability to inhibit a broad spectrum of these phosphatases. The utility of the derived compounds is illustrated with the phosphatase YopH, a bacterial toxin from Yersinia pestis. Novel chemical fragments were identified during an NMR-based screen for compounds that are capable of binding on the surface of YopH in regions adjacent the catalytic site in the presence of the spin-labeled compounds. Our data demonstrate the value of the derived chemical probes for NMR-based second-site screening in PTPs.
