Title of article :
Design and synthesis of novel photoaffinity reagents for labeling VEGF receptor tyrosine kinases
Author/Authors :
Han، نويسنده , , Sun-Young and Choi، نويسنده , , Seo Hyun and Kim، نويسنده , , Myung Hee and Lee، نويسنده , , Woo Ghil and Kim، نويسنده , , Seong Hwan and Min، نويسنده , , Yong-Ki and Kim، نويسنده , , Bum Tae، نويسنده ,
Issue Information :
هفته نامه با شماره پیاپی سال 2006
Abstract :
Novel biotin-tagged photoaffinity probes based on a trifunctional tertiary amine scaffold were synthesized and evaluated as vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. Probes 3a–c inhibit VEGF induced proliferation in HUVE cells, with IC50 values of 29.7, 33.3, and 37.7 μM, respectively. Moreover, we identified the interaction of 3b with VEGFR-2 in photoaffinity labeling experiment using HUVE cells.
Keywords :
Biotin-tagged photoaffinity probe , Inhibitor , Trifunctional probe , Vascular endothelial growth factor receptors , ligand–receptor interactions
Journal title :
Tetrahedron Letters
Journal title :
Tetrahedron Letters
