血管内皮生长因子
血管生成
酪氨酸激酶
受体酪氨酸激酶
癌症研究
血小板源性生长因子受体
激酶插入结构域受体
受体
细胞生物学
血管内皮生长因子A
血管内皮生长因子B
生物
化学
信号转导
生长因子
血管内皮生长因子受体
生物化学
作者
Samreen Ahmed,Anne Thomas,W. Steward
标识
DOI:10.1179/joc.2004.16.supplement-1.59
摘要
Angiogenesis is essential for primary tumours to grow and metastasise, and is driven by the production of positive angiogenic factors. The Vascular Endothelial Growth Factor (VEGF) family is central to the process of angiogenesis and comprises 5 molecules designated A, B, C, D and E. VEGF is overexpressed in several solid malignancies. The actions of VEGF are mediated through receptors possessing tyrosine kinase activity: VEGFR-1 (Flt-1), VEGFR-2 (Kdr/Flk-1) and VEGFR-3 (Flt-4). Anti-VEGF strategies include the use of antibodies to VEGF or its receptors, the use of ribozymes to decrease receptor expression, and the use of inhibitors of tyrosine kinase to reduce receptor activation and downstream signalling. The focus of this review is small molecule inhibitors of VEGF receptors which target their intrinsic tyrosine kinase activity. The clinical development of the following agents is discussed: SU5416, SU11248, SU6668, PTK/ZK, ZD6474.
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