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.
Keywords: Anti-Angiogenic Therapy, FGFR, Kinase Inhibitors, PDGFR, Receptor Tyrosine Kinases, VEGFR
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Published on: 29 October, 2012
Page: [335 - 346]