A review of the latest clinical compounds to inhibit VEGF in pathological angiogenesis

Sofia Baka, Andrew R. Clamp, Gordon C. Jayson

    Research output: Contribution to journalArticlepeer-review

    Abstract

    Angiogenesis plays an important role in the formation of new blood vessels and is crucial for tumour development and progression. Imbalance between pro- and antiangiogenesis factors regulates the biological process of angiogenesis. The best characterised of the proangiogenic factors and the most potent is vascular endothelial growth factor (VEGF). The binding of VEGF to one of its transmembrane tyrosine kinase receptors, which are predominantly found on endothelial cells, results in receptor dimerisation, activation and autophosphorylation of the tyrosine kinase domain. This triggers a cascade of complex downstream signalling pathways. Several strategies targeting the VEGF signalling pathway have been developed. These include neutralising antibodies to VEGF (bevacizumab) or VEGF receptors (VEGFRs) (DC101), soluble VEGFR/ VEGFR hybrids (VEGF-Trap), and tyrosine kinase inhibitors of VEGFRs (BAY43-9006, SU11248, ZD6474, AZD2171, PTK/ZK and others). Several of these agents are now being investigate in clinical trials. © 2006 Informa UK Ltd.
    Original languageEnglish
    Pages (from-to)867-876
    Number of pages9
    JournalExpert Opinion on Therapeutic Targets
    Volume10
    Issue number6
    DOIs
    Publication statusPublished - Dec 2006

    Keywords

    • Angiogenesis
    • Tyrosine kinase receptor
    • Vascular endothelial growth factor receptor

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