A Focused Library of Protein Tyrosine Phosphatase Inhibitors

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 ha...

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Veröffentlicht in:	Journal of medicinal chemistry 2010-09, Vol.53 (18), p.6768-6772
Hauptverfasser:	Comeau, Anthony B, Critton, David A, Page, Rebecca, Seto, Christopher T
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Bacterial Outer Membrane Proteins - antagonists & inhibitors Bacterial Outer Membrane Proteins - chemistry Keto Acids - chemical synthesis Keto Acids - chemistry Models, Molecular Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors Protein Tyrosine Phosphatase, Non-Receptor Type 1 - chemistry Protein Tyrosine Phosphatase, Non-Receptor Type 2 - antagonists & inhibitors Protein Tyrosine Phosphatases - antagonists & inhibitors Protein Tyrosine Phosphatases - chemistry Small Molecule Libraries Structure-Activity Relationship Yersinia pestis - enzymology
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Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm100528p