Vascular endothelial growth factor (VEGF)-A is a well-characterized angiogenic factor involved in physiological and pathological growth of blood vessels. The homologous tyrosine kinases VEGFR-1 and VEGFR-2 are the main VEGF-A receptors. Much evidence indicates that VEGF-A is important in tumor angiogenesis. Humanized anti-VEGF-A monoclonal antibodies and two small-molecule inhibitors of VEGF receptor signaling have been approved by the US Food and Drug Administration (FDA) for cancer therapy. Furthermore, VEGF-A is implicated in intraocular neovascularization associated with active proliferative retinopathies and the neovascular form of age-related macular degeneration (AMD).