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Cancer pp 333-382 | Cite as

Development of Angiogenesis Inhibitors to Vascular Endothelial Growth Factor Receptor 2 for Cancer Therapy

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Part of the Topics in Medicinal Chemistry book series (TMC, volume 1)

Abstract

Angiogenesis, the recruitment of new blood vessels, is a crucial mechanism required forboth tumor growth and metastasis. Advances in the understanding of the molecular mechanisms underlyingthe angiogenesis process have led to the discovery of a variety of pharmaceutical agents withantiangiogenic activity. The potential application of these angiogenesis inhibitors is currentlyunder intense clinical investigation. Decades of investigation suggest that vascular endothelialgrowth factor (VEGF) and its receptors, particularly VEGF receptor-2 (VEGFR-2, or kinase insert domain-containingreceptor, KDR), play a critical role in tumor-associated angiogenesis. VEGFR-2, therefore, representsa good target for therapeutic intervention. A number of agents designed selectively fortargeting VEGFR-2 are being evaluated in various phases of clinical trials in cancer patients. Thismanuscript reviews the biology of the VEGF family of ligands and receptors and of VEGFR-2 in particular.The attempts to develop effective VEGFR-2 antagonists, including small molecules, antibodies and others,for therapeutic purposes are discussed comprehensively with special emphasis on tumor angiogenesis.

Angiogenesis Angiogenesis inhibitor VEGF VEGFR KDR Tyrosine kinase inhibitors Antibody Cancer therapy 

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Copyright information

© Springer-Verlag Berlin Heidelberg 2007

Authors and Affiliations

  1. 1.Departments of Tumor Biology and Antibody TechnologyImClone Systems IncorporatedNew YorkUSA

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