Angiogenesis, the formation of new capillary blood vessels from preexisting vasculature, plays an essential role in organ growth and wound repair. However, pathological angiogenesis is a hallmark of various cancers and a range of nonneoplastic diseases including ischaemic and inflammatory disorders. Angiogenesis is a complicated multistep process that precisely mediated by the balance between pro- and antiangiogenic factors. Concentrated efforts in this area of research have led to the discovery of a growing number of angiogenesis-related molecules and the complex interactions among these molecules. The integrated understanding of molecular mechanism of angiogenesis process involved in tumor growth and metastasis has identified angiogenesis as a promising target for cancer therapy. Over the past two decades, dozens of antiangiogenic drugs have been approved for the treatment of a variety of cancers. So far, hundreds of thousands of cancer patients have benefited from antiangiogenesis treatments but limited efficacy and resistance remain outstanding problems.

This article will focus on tumor angiogenesis-related signaling molecules and pathways, development of antiangiogenic agents for the treatment of various tumors, and challenge of antiangiogenic therapy of tumors.