作者
Frank Hilberg, Gerald J Roth, Martin Krssak, Susanna Kautschitsch, Wolfgang Sommergruber, Ulrike Tontsch-Grunt, Pilar Garin-Chesa, Gerd Bader, Andreas Zoephel, Jens Quant, Armin Heckel, Wolfgang J Rettig
发表日期
2008/6/15
期刊
Cancer research
卷号
68
期号
12
页码范围
4774-4782
出版商
American Association for Cancer Research
简介
Inhibition of tumor angiogenesis through blockade of the vascular endothelial growth factor (VEGF) signaling pathway is a novel treatment modality in oncology. Preclinical findings suggest that long-term clinical outcomes may improve with blockade of additional proangiogenic receptor tyrosine kinases: platelet-derived growth factor receptors (PDGFR) and fibroblast growth factor receptors (FGFR). BIBF 1120 is an indolinone derivative potently blocking VEGF receptor (VEGFR), PDGFR and FGFR kinase activity in enzymatic assays (IC50, 20–100 nmol/L). BIBF 1120 inhibits mitogen-activated protein kinase and Akt signaling pathways in three cell types contributing to angiogenesis, endothelial cells, pericytes, and smooth muscle cells, resulting in inhibition of cell proliferation (EC50, 10–80 nmol/L) and apoptosis. In all tumor models tested thus far, including human tumor xenografts growing in nude mice and a …
引用总数
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