Niclosamide,an old antihelminthic agent,demonstrates antitumor activity by blocking multiple signaling pathways of cancer stem cells  

作　　者：Jing-Xuan Pan Ke Ding Cheng-Yan Wang 

机构地区：[1]Department of Pathophysiology,Zhongshan School of Medicine,Sun Yat-sen University,Guangzhou,Guangdong 510089,P.R.China [2]Key Laboratory of Regenerative Biology and Institute of Chemical Biology,Guangzhou Institute of Biomedicine and Health,Chinese Academy of Sciences,Guangzhou Science Park,Guangzhou,Guangdong 510089.P.R.China.

出　　处：《Chinese Journal of Cancer》2012年第4期178-184,共7页

基　　金：supported in part by grants from National Natural Science Foundation of China for Distinguished Young Scholars(81025021);the National Basic Research Program of China(973Program grant2009CB825506);the Major Research Plan of the National Natural Science Foundation of China(90713036);the National High Technology Research and Development Program of China(863Program grant2008AA02Z420);the Fundamental Research Foundation for the Central Universities to Jing-Xuan Pan

摘　　要：Niclosamide,an oral antihelminthic drug,has been used to treat tapeworm infection for about 50 years.Niclosamide is also used as a molluscicide for water treatment in schistosomiasis control programs.Recently,several groups have independently discovered that niclosamide is also active against cancer cells,but its precise mechanism of antitumor action is not fully understood.Evidence supports that niclosamide targets multiple signaling pathways (NF-κB,Wnt/β-catenin,Notch,ROS,mTORC1,and Stat3),most of which are closely involved with cancer stem cells.The exciting advances in elucidating the antitumor activity and the molecular targets of this drug will be discussed.A method for synthesizing a phosphate pro-drug of niclosamide is provided.Given its potential antitumor activity,clinical trials for niclosamide and its derivatives are warranted for cancer treatment.Niclosamide, an oral antihelminthic drug, has been used to treat tapeworm infection for about 50 years. Niclosamide is also used as a molluscicide for water treatment in schistosomiasis control programs. Recently, several groups have independently discovered that niclosamide is also active against cancer cells, but its precise mechanism of antitumor action is not fully understood. Evidence supports that niclosamide targets multiple signaling pathways （NF-KB, Wnt/13-catenin, Notch, RQS, mTORC1, and Stat3）, most of which are closely involved with cancer stem cells. The exciting advances in elucidating the antitumor activity and the molecular targets of this drug will be discussed. A method for synthesizing a phosphate pro-drug of niclosamide is provided. Given its potential antitumor activity, clinical trials for niclosamide and its derivatives are warranted for cancer treatment.

关 键 词：抗肿瘤活性 氯硝柳胺 信号转导途径 干细胞 癌症 驱虫剂 显示 杀软体动物剂 

分 类 号：Q255[生物学—细胞生物学] TQ463.5[化学工程—制药化工]