A Focused Library of Protein Tyrosine Phosphatase Inhibitors

作者：Comeau Anthony B; Critton David A; Page Rebecca; Seto Christopher T^*

来源：Journal of Medicinal Chemistry, 2010, 53(18): 6768-6772.

DOI：10.1021/jm100528p

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 a-ketoacid-based inhibitors has been screened against several tyrosine phosphatases. Compound 2a has IC(50) 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.

• 出版日期2010-9-23