Abstract
We report here a class of thiazolidine-2,4-diones and 2-thioxothiazolidin-4-ones as potent inhibitors of the lymphoid specific tyrosine phosphatase (Lyp) identified from high throughput screens. Chemical modification by incorporating the known phosphotyrosine (pTyr) mimics led to the discovery of a salicylate-based inhibitor with submicromolar potency.
MeSH terms
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Binding Sites
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology*
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Models, Chemical
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Molecular Mimicry
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Phosphotyrosine / chemistry
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Protein Tyrosine Phosphatase, Non-Receptor Type 22 / antagonists & inhibitors*
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Protein Tyrosine Phosphatases / antagonists & inhibitors*
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Structure-Activity Relationship
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Thiazolidinediones / chemical synthesis
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Thiazolidinediones / pharmacology*
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Thiazolidines / chemical synthesis
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Thiazolidines / pharmacology*
Substances
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Enzyme Inhibitors
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Thiazolidinediones
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Thiazolidines
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Phosphotyrosine
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Protein Tyrosine Phosphatase, Non-Receptor Type 22
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Protein Tyrosine Phosphatases