Abstract
By replacing the phosphate group in pTyr with an isoxazole carboxylic acid, a novel unnatural amino acid has been successfully synthesized. Subsequently, its incorporation into a known PPI (protein-protein interaction) inhibitor of STAT3 protein (ISS 610) generated I2 which showed reasonable anti-STAT3 activity in both fluorescence polarization and cell-proliferation experiments.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acids / chemistry*
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Animals
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Carboxylic Acids / chemical synthesis
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Carboxylic Acids / chemistry
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Cell Line
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Cell Proliferation
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Fluorescence Polarization
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Humans
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Isoxazoles / chemistry
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Mice
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Phosphotyrosine / chemistry*
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Protein Binding
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STAT3 Transcription Factor / antagonists & inhibitors
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STAT3 Transcription Factor / metabolism
Substances
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Amino Acids
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Carboxylic Acids
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Isoxazoles
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STAT3 Transcription Factor
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Phosphotyrosine