Angiogenesis plays a critical role in tissue development, reproduction and repair in both health and disease. Pathologically, tumorigenesis relies heavily on angiogenesis for vascularization to extract necessary nutrients and oxygen from the local microenvironment to support tumor growth. The development of anti-angiogenic agents has become an attractive drug discovery strategy for anti-cancer therapy. Targeting signal transduction pathway components currently serves as one of the most validated therapeutic development approaches among all of the other druggable factors in the complicated tumor microenvironment. In this respect, kinase inhibitors interfering with critical regulators of angiogenesis such as VEGFR and PDGFR have provided valuable information from preclinical and clinical perspectives. Herein, we summarize the recent efforts towards the development of kinase inhibitors that target a variety of signaling pathway nodes in the angiogenesis process from both drug discovery and pharmacological points of view in order to provide an overview of their current applications and future development.

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