Squaric Acids:  A New Motif for Designing Inhibitors of Protein Tyrosine Phosphatases

Squaric Acids:  A New Motif for Designing Inhibitors of Protein Tyrosine Phosphatases

Protein tyrosine phosphatases (PTPases) are important targets in medicinal chemistry. These enzymes play a role in a number of human diseases, including type II diabetes and infection by Yersinia pestis, the causative agent of bubonic plague. Derivatives of squaric acids such as 2-aryl-1-hydroxycycl...

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Veröffentlicht in:Organic letters 2004-01, Vol.6 (1), p.83-86
Hauptverfasser: Xie, Jian, Comeau, Anthony B, Seto, Christopher T
Format: Artikel
Sprache:eng
Schlagworte:
Amides - chemistry
Amides - pharmacology
Cyclobutanes - chemistry
Cyclobutanes - pharmacology
Drug Design
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Humans
Models, Chemical
Molecular Structure
Protein Tyrosine Phosphatases - antagonists & inhibitors
Protein Tyrosine Phosphatases - chemistry
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Zusammenfassung:Protein tyrosine phosphatases (PTPases) are important targets in medicinal chemistry. These enzymes play a role in a number of human diseases, including type II diabetes and infection by Yersinia pestis, the causative agent of bubonic plague. Derivatives of squaric acids such as 2-aryl-1-hydroxycyclobut-1-ene-3,4-diones represent a new class of monoanionic inhibitors for PTPases.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol036121w