J-4: a novel and typical preclinical anticancer drug targeting protein   kinase C zeta

doi:10.1097/CAD.0b013e3283514cc1

CORC > 北京大学 > 化学与分子工程学院

	J-4: a novel and typical preclinical anticancer drug targeting protein kinase C zeta
	Li, Hongyan ; Wu, Jing ; Ying, Guoguang ; Chen, Liwei ; Lai, Luhua ; Liu, Zhe ; Zhang, Ning ; Guo, Hua
刊名	anti cancer drugs
	2012
关键词	breast cancer chemotaxis epidermal growth factor J-4 protein kinase C zeta BREAST-CANCER CELLS CHEMOTAXIS SIGNAL-TRANSDUCTION PKC-ZETA ACTIN POLYMERIZATION ACTIVATION MOTILITY ADHESION CDC42
DOI	10.1097/CAD.0b013e3283514cc1
英文摘要	Metastasis is the major cause of morbidity and mortality from breast cancer. Cell motility and chemotaxis play important roles in the metastatic cascade of cancer cells. Protein kinase C zeta (PKC zeta) mediates cancer cell chemotaxis by regulating cytoskeleton rearrangement and cell adhesion. In the current study, we investigated the inhibitory effect of a compound called J-4 targeting PKC zeta. J-4 was tested with inhibitory concentration (IC50) of 10 mu mol/l using a Z'-LYTE (TM) Kinase Assay-Ser/Thr 7 Peptide Kit. Our results show that J-4 inhibited spontaneous migration and epidermal growth factor (EGF)-induced chemotaxis of human breast cancer cell MDA-MB-231. Through an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, the drug designated as J-4 had no obvious cytotoxicity in vitro. Meanwhile, in the presence of J-4, the cells showed defects in EGF-induced actin polymerization and adhesion. Furthermore, J-4 dampened EGF-induced phosphorylation and recycling of cofilin. Taken together, our data demonstrate that J-4 is a new and typical inhibitor that blocks the PKC zeta pathway. Moreover, a better understanding of the mechanism of action of J-4 may provide a novel medical therapeutic strategy for cancer treatment that would block metastasis, thereby reducing the proliferation and dissemination of cancer cells and increasing patient survival. Anti-Cancer Drugs 23:691-697 (C) 2012 Wolters Kluwer Health vertical bar Lippincott Williams & Wilkins.; Oncology; Pharmacology & Pharmacy; SCI(E); 0; ARTICLE; 7; 691-697; 23
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/393137]
专题	化学与分子工程学院
推荐引用方式 GB/T 7714	Li, Hongyan,Wu, Jing,Ying, Guoguang,et al. J-4: a novel and typical preclinical anticancer drug targeting protein kinase C zeta[J]. anti cancer drugs,2012.
APA	Li, Hongyan.,Wu, Jing.,Ying, Guoguang.,Chen, Liwei.,Lai, Luhua.,...&Guo, Hua.(2012).J-4: a novel and typical preclinical anticancer drug targeting protein kinase C zeta.anti cancer drugs.
MLA	Li, Hongyan,et al."J-4: a novel and typical preclinical anticancer drug targeting protein kinase C zeta".anti cancer drugs (2012).