Abstract
Several 'classical' protein tyrosine phosphatases are attractive therapeutic targets, including PTP1B for obesity and Type II diabetes; SHP2 for cancer and Lyp for rheumatoid arthritis. Progress has been made in identifying a broad range of chemically distinct inhibitors; however, developing selective and cell-permeable clinically useful compounds has proved challenging. Here the ongoing challenges and recent significant advances in the field are reviewed. Key novel compounds are highlighted and a perspective on the future of phosphatase inhibitor development is presented.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Autoimmune Diseases / drug therapy
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Autoimmune Diseases / enzymology
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Diabetes Mellitus, Type 2 / drug therapy
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Diabetes Mellitus, Type 2 / enzymology
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Drug Discovery / methods*
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology*
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Enzyme Inhibitors / therapeutic use
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Humans
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Models, Molecular
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Neoplasms / drug therapy
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Neoplasms / enzymology
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Obesity / drug therapy
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Obesity / enzymology
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Protein Tyrosine Phosphatases / antagonists & inhibitors*
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Protein Tyrosine Phosphatases / chemistry
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Protein Tyrosine Phosphatases / metabolism*
Substances
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Enzyme Inhibitors
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Protein Tyrosine Phosphatases