C11, a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor, suppresses breast cancer metastasis and angiogenesis

doi:10.1038/s41401-018-0191-7

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第一研究室

	C11, a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor, suppresses breast cancer metastasis and angiogenesis
	Chen, Zhuo 2; Tong, Lin-Jiang 2; Tang, Bai-You 2; Liu, Hong-Yan 2; Wang, Xin1 ; Zhang, Tao 2; Cao, Xian-Wen 1; Chen, Yi2 ; Li, Hong-Lin 1; Qian, Xu-Hong 1
刊名	Acta pharmacologica Sinica
	2018-11-28
ISSN号	1745-7254
DOI	10.1038/s41401-018-0191-7
文献子类	Article
英文摘要	The fibroblast growth factor receptors (FGFRs) are increasingly considered attractive targets for therapeutic cancer intervention due to their roles in tumor metastasis and angiogenesis. Here, we identified a new selective FGFR inhibitor, C11, and assessed its antitumor activities. C11 was a selective FGFR1 inhibitor with an IC of 19 nM among a panel of 20 tyrosine kinases. C11 inhibited cell proliferation in various tumors, particularly bladder cancer and breast cancer. C11 also inhibited breast cancer MDA-MB-231 cell migration and invasion via suppression of FGFR1 phosphorylation and its downstream signaling pathway. Suppression of matrix metalloproteinases 2/9 (MMP2/9) was associated with the anti-motility activity of C11. Furthermore, the anti-angiogenesis activity of C11 was verified in endothelial cells and chicken chorioallantoic membranes (CAMs). C11 inhibited the migration and tube formation of HMEC-1 endothelial cells and inhibited angiogenesis in a CAM assay. In sum, C11 is a novel selective FGFR1 inhibitor that exhibits potent activity against breast cancer metastasis and angiogenesis.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/266683]
专题	药理学第一研究室
通讯作者	Xu, Yu-Fang; Xie, Hua; Ding, Jian
作者单位	1.Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai, 200237, China 2.Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China;
推荐引用方式 GB/T 7714	Chen, Zhuo,Tong, Lin-Jiang,Tang, Bai-You,et al. C11, a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor, suppresses breast cancer metastasis and angiogenesis[J]. Acta pharmacologica Sinica,2018.
APA	Chen, Zhuo.,Tong, Lin-Jiang.,Tang, Bai-You.,Liu, Hong-Yan.,Wang, Xin.,...&Ding, Jian.(2018).C11, a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor, suppresses breast cancer metastasis and angiogenesis.Acta pharmacologica Sinica.
MLA	Chen, Zhuo,et al."C11, a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor, suppresses breast cancer metastasis and angiogenesis".Acta pharmacologica Sinica (2018).