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A Focused Library of Protein Tyrosine Phosphatase Inhibitors

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journal contribution
posted on 23.09.2010, 00:00 by Anthony B. Comeau, David A. Critton, Rebecca Page, Christopher T. Seto
Protein tyrosine phosphatases such as PTP1B and YopH are potential targets for the development of therapeutic agents against a variety of pathological conditions including diabetes, obesity, and infection by the bacterium Yersinia pestis. A focused library of bidentate α-ketoacid-based inhibitors has been screened against several tyrosine phosphatases. Compound 2a has IC50 values of 43 and 220 nM against YopH and PTP1B, respectively, and shows a 30-fold selectivity for PTP1B over the closely related phosphatase TCPTP.