Abstract
A novel biotin-tagged photoaffinity probe was synthesized and evaluated as a vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor. The probe (2) is a potent VEGFR-2 inhibitor with an IC(50) value of 7.1 microM, and inhibits VEGF-induced proliferation in human umbilical vein endothelial cells (HUVEC), with an IC(50) value of 40.3 microM. This probe will be a useful reagent for investigating ligand-protein interactions.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Biotin / chemistry*
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Cell Proliferation
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Cells, Cultured
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Endothelial Cells / cytology
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Endothelium, Vascular / cytology
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Humans
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Hydrocarbons, Brominated / chemistry
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Inhibitory Concentration 50
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Ligands
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Light
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Models, Chemical
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Protein Binding
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Quinazolines / chemistry
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Receptors, Vascular Endothelial Growth Factor / chemistry*
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Receptors, Vascular Endothelial Growth Factor / metabolism
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Spectrophotometry, Ultraviolet
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Thiazoles / chemistry
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Time Factors
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Ultraviolet Rays
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Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors
Substances
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2,4-dibromo-5-hydroxymethylthiazole
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Hydrocarbons, Brominated
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Ligands
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Quinazolines
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Thiazoles
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Biotin
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Receptors, Vascular Endothelial Growth Factor
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Vascular Endothelial Growth Factor Receptor-2