A novel non-ATP competitive FGFR1 inhibitor with therapeutic potential on gastric cancer through inhibition of cell proliferation, survival and migration

doi:10.1007/s10495-017-1361-7

科研成果详情

题名	A novel non-ATP competitive FGFR1 inhibitor with therapeutic potential on gastric cancer through inhibition of cell proliferation, survival and migration
作者	Wu, Jianzhang1; Du, Xiaojing2; Li, Wulan1,3; Zhou, Yangyang1,2; Bai, Encheng1,2; Kang, Yanting 1,2; Chen, Qiuxiang1,2; Fu, Weitao 1; Yun, Di 1; Xu, Qing 4; Qiu, Peihong 1; Jin, Rong2,5; Cai, Yuepiao1; Liang, Guang1
发表日期	2017-06
发表期刊	APOPTOSIS 影响因子和分区
语种	英语
原始文献类型	Article
关键词	Gastric cancer Non-ATP competitive FGFR1 inhibitor Proliferation Survival Migration
其他关键词	FACTOR RECEPTOR 1 ; GROWTH-FACTOR RECEPTORS ; GENE AMPLIFICATION ; LUNG-CANCER ; DISCOVERY ; EXPRESSION ; TARGET
摘要	Fibroblast growth factor receptor 1 (FGFR1), belonging to receptor tyrosine kinases (RTKs), possesses various biological functions. Over-expression of FGFR1 has been observed in multiple human malignancies. Hence, targeting FGFR1 is an attractive prospect for the advancement of cancer treatment options. Here, we present a novel small molecular FGFR1 inhibitor L16H50, which can inhibit FGFR1 kinase in an ATP-independent manner. It potently inhibits FGFR1-mediated signaling in a gastric cancer cell line, resulting in inhibition of cell growth, survival and migration. It also displays an outstanding anti-tumor activity in a gastric cancer xenograft tumor model by targeting FGFR1 signaling. These results show that L16H50 is a potent non-ATP-competitive FGFR1 inhibitor and may provide strong rationale for its evaluation in gastric cancer patients.
资助项目	National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81402839, 81473242, 81272462]; ZheJiang Province Natural Science Fund of China [LY17H160059, LY14H160044]; Technology Foundation for Medical Science of Zhejiang Province [2012KYA129]; Opening Project of Zhejiang Provincial Top Key Discipline of Pharmaceutical Sciences
出版者	SPRINGER
出版地	DORDRECHT
ISSN	1360-8185
EISSN	1573-675X
卷号	22 期号:6 页码:852-864
DOI	10.1007/s10495-017-1361-7
页数	13
WOS类目	Biochemistry & Molecular Biology ; Cell Biology
WOS研究方向	Biochemistry & Molecular Biology ; Cell Biology
WOS记录号	WOS:000399883500010
收录类别	SCIE ; PUBMED ; SCOPUS
URL	查看原文
PubMed ID	28315172
SCOPUSEID	2-s2.0-85015706027
通讯作者地址	[Qiu, Peihong]Chemical Biology Research Center,College of Pharmaceutical Sciences,Wenzhou Medical Universtiy,Wenzhou,325035,China
Scopus学科分类	Pharmacology;Pharmaceutical Science;Clinical Biochemistry;Cell Biology;Biochemistry (medical);Cancer Research
引用统计	被引频次：8[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	https://kms.wmu.edu.cn/handle/3ETUA0LF/18327
专题	药学院（分析测试中心）附属第一医院药学院（分析测试中心）_生物有机与药物化学研究中心第一临床医学院（信息与工程学院）、附属第一医院_计算机与信息管理系
通讯作者	Qiu, Peihong
作者单位	1.Chemical Biology Research Center,College of Pharmaceutical Sciences,Wenzhou Medical Universtiy,Wenzhou,325035,China; 2.Department of Digestive Diseases,The First Affiliated Hospital of Wenzhou Medical University,Wenzhou,325000,China; 3.College of Information Science and Computer Engineering,the First Clinical Medical College,Wenzhou Medical University,Wenzhou,325035,China; 4.College of Chemistry and Materials Engineering,Wenzhou University,Wenzhou,325035,China; 5.Department of Epidemiology,The First Affiliated Hospital of Wenzhou Medical University,Wenzhou,325000,China
第一作者单位	生物有机与药物化学研究中心
通讯作者单位	生物有机与药物化学研究中心
第一作者的第一单位	生物有机与药物化学研究中心
推荐引用方式 GB/T 7714	Wu, Jianzhang,Du, Xiaojing,Li, Wulan,et al. A novel non-ATP competitive FGFR1 inhibitor with therapeutic potential on gastric cancer through inhibition of cell proliferation, survival and migration[J]. APOPTOSIS,2017,22(6):852-864.
APA	Wu, Jianzhang., Du, Xiaojing., Li, Wulan., Zhou, Yangyang., Bai, Encheng., ... & Liang, Guang. (2017). A novel non-ATP competitive FGFR1 inhibitor with therapeutic potential on gastric cancer through inhibition of cell proliferation, survival and migration. APOPTOSIS, 22(6), 852-864.
MLA	Wu, Jianzhang,et al."A novel non-ATP competitive FGFR1 inhibitor with therapeutic potential on gastric cancer through inhibition of cell proliferation, survival and migration".APOPTOSIS 22.6(2017):852-864.