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Exp Mol Med ; 38(5): 502-8, 2006 Oct 31.
Article in English | MEDLINE | ID: mdl-17079866

ABSTRACT

Angiogenesis is considered to be an integral process to the growth and spread of solid tumors. Anti-angiogenesis therapy recently has been found to be one of the most promising anti-cancer therapeutic strategies. In this study, we provide several lines of evidences showing that KR-31831, a new benzopyran derivative, has anti-angiogenic activities. KR-31831 inhibited the proliferation, migration, invasion and tube formation of bovine aortic endothelial cells (BAECs), and suppressed the release of matrix metalloproteinase-2 (MMP-2) of BAECs. KR-31831 also inhibited in vivo angiogenesis in mouse Matrigel plug assay. Furthermore, the mRNA expressions of basic fibroblast growth factor (bFGF), fibroblast growth factor receptor-2 (FGFR-2), and vascular endothelial growth factor receptor-2 (VEGFR-2) were decreased by KR-31831. Taken together, these results suggest that KR-31831 acts as a novel angiogenesis inhibitor and might be useful for treating hypervascularized cancers.


Subject(s)
Angiogenesis Inhibitors/pharmacology , Benzopyrans/pharmacology , Imidazoles/pharmacology , Neovascularization, Pathologic/drug therapy , Angiogenesis Inhibitors/therapeutic use , Animals , Benzopyrans/therapeutic use , Cattle , Cell Movement/drug effects , Cells, Cultured , Endothelial Cells/drug effects , Fibroblast Growth Factor 2/metabolism , Imidazoles/therapeutic use , In Vitro Techniques , Ischemia/drug therapy , Male , Matrix Metalloproteinase 2/metabolism , Mice , Mice, Inbred C57BL , Models, Biological , Neovascularization, Physiologic/drug effects , Receptor, Fibroblast Growth Factor, Type 2/metabolism , Vascular Endothelial Growth Factor Receptor-2/metabolism
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