A Focused Library of Protein Tyrosine Phosphatase Inhibitors

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• 作者：Anthony B. Comeau ; David A. Critton ; Rebecca Page ; Christopher T. Seto
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：September 23, 2010
• 年：2010
• 卷：53
• 期：18
• 页码：6768-6772
• 全文大小：841K
• 年卷期：v.53,no.18(September 23, 2010)
• ISSN：1520-4804

文摘

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.