Fluacrypyrim, a novel STAT3 activation inhibitor, induces cell cycle arrest and apoptosis in cancer cells harboring constitutively-active STAT3

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	Fluacrypyrim, a novel STAT3 activation inhibitor, induces cell cycle arrest and apoptosis in cancer cells harboring constitutively-active STAT3
	Yu, Zu-Yin ; Huang, Rui ; Xiao, He ; Sun, Wen-Feng ; Shan, Ya-Jun ; Wang, Bo ; Zhao, Ting-Ting ; Dong, Bo ; Zhao, Zhen-Hu ; Liu, Xiao-Lan ; Wang, Sheng-Qi ; Yang, Ri-Fang ; Luo, Qing-Liang ; Cong, Yu-Wen ; Huang R(黄蕊)
刊名	http://dx.doi.org/10.1002/ijc.25169
	2010-09-15
关键词	MULTIPLE-MYELOMA CELLS G-QUARTET OLIGONUCLEOTIDES POTENT ANTITUMOR-ACTIVITY TUMOR IN-VIVO SIGNAL TRANSDUCER SUPPRESSES GROWTH TRANSCRIPTION FACTORS MOLECULAR TARGETS GENE-REGULATION BREAST-TUMORS
英文摘要	National Sciences Fund [90713031, 30701028]; STAT3 protein has an important role in oncogenesis and is a promising anticancer target. Herein, we demonstrate that a novel small molecule fluacrypyrim (FAPM) inhibits the growth of leukemia cells by a predominant G1 arrest with significant decrease of the protein and mRNA levels of cyclin Dl. As cyan D1 is transcriptionally regulated by STAT3, FAPM is then shown to markedly inhibit the STAT3 phosphorylation with marginal effect on the other signal transducers and activators of transcription, and without effect on phosphoinositide-3-kinase and mitogen-activated protein kinase pathways. Further analysis shows that FAPM significantly increases the protein tyrosine phosphatases (PTPs) activity in a dose-dependent manner, and the inhibition of PIP activation by sodium pervanadate reverses FAPM-induced suppression of STAT3 tyrosine phosphorylation, indicating an important role of PTP in the action of FAPM. Finally, FAPM treatment results in selective suppression of STAT3-mediated transcriptional activity and its downstream effectors, and subsequent induction of growth arrest and apoptosis in STAT3-dependent cancer cell lines. This study therefore identifies FAPM as a potent STAT3 activation inhibitor with possible therapeutic potential against malignancies with constitutive STAT3 activation.
语种	英语
出版者	INT J CANCER
内容类型	期刊论文
源URL	[http://dspace.xmu.edu.cn/handle/2288/91598]
专题	物理技术－已发表论文
推荐引用方式 GB/T 7714	Yu, Zu-Yin,Huang, Rui,Xiao, He,et al. Fluacrypyrim, a novel STAT3 activation inhibitor, induces cell cycle arrest and apoptosis in cancer cells harboring constitutively-active STAT3[J]. http://dx.doi.org/10.1002/ijc.25169,2010.
APA	Yu, Zu-Yin.,Huang, Rui.,Xiao, He.,Sun, Wen-Feng.,Shan, Ya-Jun.,...&黄蕊.(2010).Fluacrypyrim, a novel STAT3 activation inhibitor, induces cell cycle arrest and apoptosis in cancer cells harboring constitutively-active STAT3.http://dx.doi.org/10.1002/ijc.25169.
MLA	Yu, Zu-Yin,et al."Fluacrypyrim, a novel STAT3 activation inhibitor, induces cell cycle arrest and apoptosis in cancer cells harboring constitutively-active STAT3".http://dx.doi.org/10.1002/ijc.25169 (2010).