Translational Medicine
Open Access

Abstract

Landscape and Targeting of the Angpt-Tie System in Current Anticancer Therapy

LYu Sun and Boyi Zhang

Strategies using angiogenesis inhibitors to suppress tumor development via interfering with vascular signaling have been explored for more than a decade. To date, anti-angiogenenic agents such as bevacizumab, sorafenib and sunitinib are incorporated into standard administration to treat many cancer types by targeting the vascular endothelial growth factor A (VEGFA) pathway. However, only mild and transient responses were observed in most cases, raising the topic of drug resistance as one of the major problems that is frequently encountered by clinicians. The angiopoietin (Angpt)-Tie system, previously considered as a second line pathway in tumor angiogenic switch that functionally contributes to angiogenesis and/or lymphangiogenesis, recently attracted substantial interest and is entering the spotlight for meticulous studies in cancer biology. Agents specifically suppressing Angpts are now in clinical trials, and new reports suggest promising anti-cancer activities with a safety profile distinct from those of anti- VEGFA therapeutics. This review provides an updated picture of the Angpt-Tie system, by focusing on the Angpt-Tie2 axis in basic research and clinical investigation, and discusses feasible options to therapeutically target this signaling pathway in the context of precision medicine.