DEVELOPMENT OF A HIGH THROUGHPUT ASSAY FOR VEGFR2 INHIBITION

Over-expression of Vascular Endothelial Growth Factor-A (VEGF-A) can lead to a variety of human diseases, including different forms of cancer, psoriasis, and arthritis. The goal of this project was to develop a cell culture-based assay using human umbilical vein endothelial cells (HUVECs) to identify potential inhibitors of the VEGF-Receptor-2 (VEGFR2) and potential blockers of angiogenesis. After testing a variety of assays, the Hoechst nuclear stain was found to be convenient assays for quantifying cell proliferation. A screen of a chemical compound library using this Hoechst assay identified BSB660 as a novel inhibitor of VEGFR2. In the future, other chemical libraries will be tested using a TDA in vitro assay under development by other Blue Sky employees