Vascular endothelial growth factor (VEGF) inhibition by small molecules.

作者: S.I. Ahmed , A.L. Thomas , W.P. Steward

DOI: 10.1179/JOC.2004.16.SUPPLEMENT-1.59

关键词: FLT4Kinase insert domain receptorBiochemistryVascular endothelial growth factorAngiogenesisPlatelet-derived growth factor receptorVascular endothelial growth factor ACancer researchChemistryReceptor tyrosine kinaseTropomyosin receptor kinase C

摘要: Angiogenesis is essential for primary tumours to grow and metastasise, driven by the production of positive angiogenic factors. The Vascular Endothelial Growth Factor (VEGF) family central process angiogenesis comprises 5 molecules designated A, B, C, D E. VEGF overexpressed in several solid malignancies. actions are mediated through receptors possessing tyrosine kinase activity: VEGFR-1 (Flt-1), VEGFR-2 (Kdr/Flk-1) VEGFR-3 (Flt-4). Anti-VEGF strategies include use antibodies or its receptors, ribozymes decrease receptor expression, inhibitors reduce activation downstream signalling. focus this review small molecule which target their intrinsic activity. clinical development following agents discussed: SU5416, SU11248, SU6668, PTK/ZK, ZD6474.

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