Lou Huiping, Gao Yanfeng, Zhai Mingxia, Qi Yuanming, Chen Lixiang, Lv Hong, Yu Jibing, Li Yongxin
Department of Bioengineering, Zhengzhou University, Science Road 100, Zhengzhou 450001, China.
Bioorg Med Chem Lett. 2008 Aug 15;18(16):4633-7. doi: 10.1016/j.bmcl.2008.07.017. Epub 2008 Jul 10.
A series of novel peptides from various motifs of Asterina pectinifera cyclin B and their derivatives conjugated to HIV-Tat(49-57) were designed and synthesized. Their bioactivities on two human cancer cell lines were determined. Among them, Tat-a5 (KAQIRAMECNILGRKKRRQRRR) exhibited significant cytotoxic effects on cancer cell lines EC-9706 and HCT-116. Tat-a5 could arrest cancer cells at G(2)/M phase and make them apoptotic. Our results suggested that Tat-a5 could be a novel leading peptide with anticancer activity.
设计并合成了一系列来自海盘车细胞周期蛋白B不同基序的新型肽及其与HIV-Tat(49-57)偶联的衍生物。测定了它们对两种人类癌细胞系的生物活性。其中，Tat-a5（KAQIRAMECNILGRKKRRQRRR）对癌细胞系EC-9706和HCT-116表现出显著的细胞毒性作用。Tat-a5可使癌细胞停滞于G(2)/M期并使其凋亡。我们的结果表明，Tat-a5可能是一种具有抗癌活性的新型先导肽。
