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

被引：77

作者：

Baka, Sofia ^{[1
]}

Clamp, Andrew R. ^{[1
]}

Jayson, Gordon C. ^{[1
]}

机构：

[1] Christie Hosp NHS Trust, Manchester M20 4BX, Lancs, England

来源：

EXPERT OPINION ON THERAPEUTIC TARGETS | 2006年 / 10卷 / 06期

基金：

英国医学研究理事会;

关键词：

angiogenesis; tyrosine kinase receptor; vascular endothelial growth factor receptor;

D O I：

10.1517/14728222.10.6.867

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 investigated in clinical trials.

引用

页码：867 / 876

页数：10

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