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2015 ; 8
(9
): 10355-64
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Xanthatin, a novel potent inhibitor of VEGFR2 signaling, inhibits angiogenesis
and tumor growth in breast cancer cells
#MMPMID26617743
Yu Y
; Yu J
; Pei CG
; Li YY
; Tu P
; Gao GP
; Shao Y
Int J Clin Exp Pathol
2015[]; 8
(9
): 10355-64
PMID26617743
show ga
Anti-angiogenesis targeting vascular endothelial growth factor receptor 2
(VEGFR2) has emerged as an important tool for cancer treatment. In this study, we
described a novel VEGFR2 inhibitor, xanthatin, which inhibits tumor angiogenesis
and growth. The biochemical profiles of xanthatin were investigated using kinase
assay, migration assay, tube formation, Matrigel plug assay, western blot,
immunofluorescence and human tumor xenograft model. Xanthatin significantly
inhibited growth, migration and tube formation of human umbilical vascular
endothelial cell as well as inhibited vascular endothelial growth factor
(VEGF)-stimulated angiogenesis. In addition, it inhibited VEGF-induced
phosphorylation of VEGFR2 and its downstream signaling regulator. Moreover,
xanthatin directly inhibit proliferation of breast cancer cells MDA-MB-231. Oral
administration of xanthatin could markedly inhibit human tumor xenograft growth
and decreased microvessel densities (MVD) in tumor sections. Taken together,
these preclinical evaluations suggest that xanthatin inhibits angiogenesis and
may be a promising anticancer drug candidate.