Integrin-Mediated Delivery of Drugs and Nucleic Acids for Anti-Angiogenic Cancer Therapy: Current Landscape and Remaining Challenges

Abstract

Angiogenesis, sprouting of new blood vessels from pre-existing vasculatures, plays a critical role in regulating tumor growth. Binding interactions between integrin, a heterodimeric transmembrane glycoprotein receptor, and its extracellular matrix (ECM) protein ligands govern the angiogenic potential of tumor endothelial cells. Integrin receptors are attractive targets in cancer therapy due to their overexpression on tumor endothelial cells, but not on quiescent blood vessels. These receptors are finding increasing applications in anti-angiogenic therapy via targeted delivery of chemotherapeutic drugs and nucleic acids to tumor vasculatures. The current article attempts to provide a retrospective account of the past developments, highlight important contemporary contributions and unresolved set-backs of this emerging field.