Table 1

Antiangiogenic and vascular targeting agents: target and activity

AgentTargetActivity
TNP-40Protein myristoylation and dependent signaling pathways in endothelial cellsUp-regulation of apoptotic pathways in endothelial cells
AngiostatinEndothelial cell membrane receptor (possibly membrane proton pump)Inhibition of pH regulation and up-regulation of apoptotic pathways in endothelial cells
VEGF/VEGFR inhibitorsNeovascularization processes; endothelial cell survival pathways; tumor cell survival pathways indirectly and possibly directly through autocrine signaling loopsInhibition of endothelial cell migration, tube formation, etc.; up-regulation of apoptosis in endothelial cells through down-regulation of key signaling molecules, i.e. survivin, BCL-2
COX-2 inhibitorsProstaglandin synthesisInhibition of VEGF synthesis in tumor cells; up-regulation of apoptotic signaling pathways in tumor cells and endothelial cells
EGFR inhibitorsVEGF synthesis, apoptotic signaling in tumor cells and endothelial cellsInhibition of tumor angiogenesis; up-regulation of apoptosis in both tumor cells and endothelial cells
Vascular targeting agents (i.e. ZD6126)Microtubular cytoskeleton in endothelial cellsVasculature shutdown leading to tumor necrosis