Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases

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 IC50 value of 7.1 μM, and inhibits VEGF-induced proliferation in human umbilical vein endothelial cells (HUVEC), with an IC50 value of 40.3 μM. This probe will be a useful reagent for investigating ligand–protein interactions.

A novel biotin-tagged photoaffinity probe (2) was synthesized and evaluated as a vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor.Figure optionsDownload as PowerPoint slide