Development of novel angiogenesis inhibitors targeting VEGF (vascular endothelial growth factor) for cancer chemotherapy

Recent progress in cancer biology has revealed that angiogenesis is a promising target for new anticancer drugs. Angiogenesis is tightly regulated by the balance between stimulatory and inhibitory angiogenic factors, and the imbalance of these regulators causes dysfunction of angiogenesis. Vascular endothelial growth factor (VEGF) is one of the best characterized pro-angiogenic factors, and multiple strategies have been studied to inhibit the pathway; i. e. production and secretion of VEGF receptor, VEGF binding to its receptor, tyrosine kinase activity of VEGF, and signaling pathway downstream induced by VEGF. In this article, the summary of function of VEGF family as well as recent promising drugs under clinical trials including bevacizumab (Avastin), a humanized monoclonal antibody developed against VEGF, and several small molecule inhibitors targeting VEGF function are described.