IMR Press / FBL / Volume 10 / Issue 2 / DOI: 10.2741/1629

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.

Open Access Article
Development of angiogenesis inhibitors to vascular endothelial growth factor receptor 2. Current status and future perspective
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1 Department of Antibody Technology, ImClone Systems Incorporated, New York, NY 10014, USA

Academic Editor: Yiwen Li

Front. Biosci. (Landmark Ed) 2005, 10(2), 1415–1439;
Published: 1 May 2005
(This article belongs to the Special Issue Tumor angiogenesis)

Angiogenesis, the recruitment of new blood vessels is a crucial mechanism required for both tumor growth and metastasis. Advances in the understanding of the molecular mechanisms underlying the angiogenesis process have led to the discovery of a variety of pharmaceutical agents with antiangiogenic activity. The potential application of these angiogenesis inhibitors is currently under intense clinical investigation. Decades of investigation suggest that vascular endothelial growth factor (VEGF) and its receptors, particularly VEGF receptor 2 (VEGFR2, or kinase insert domain-containing receptor, KDR), play a critical role in tumor-associated angiogenesis. KDR, therefore, represents a good target for therapeutic intervention. A number of agents designed selectively for targeting KDR are being evaluated in various phases of clinical trials in cancer patients. This manuscript reviews briefly the biology of VEGF family of ligands and receptors and of KDR in particular. The attempts to develop effective KDR antagonists, including small molecules, antibodies and others, for therapeutic purposes are discussed comprehensively with special emphasis on tumor angiogenesis.

Angiogenesis Inhibitor
Tyrosine Kinase Inhibitors
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