WONG, KA LEUNG,黄 嘉良,黃 嘉良,MAK, NAI KI,麦 乃岐,麥 乃岐,JIANG, LI JUN,江丽君,江麗君
申请号：
TW106113830
公开号：
TW201739471A
申请日:
2017.04.25
申请国别(地区):
TW
年份:
2017
代理人:
摘要：
This invention provides a nucleus-permeable small-molecule inhibitor,L2P4(whereL2is4-(4-(Diethylamino)styryl)-N-carboxymethylpyridinium chlorideandP4is an amino acid sequence comprisingCAhxYFMVFGGRrRKandthey were coupled through amide bond) and synthesis thereof, which effectively targets the dimerization interface of EBNA1, a critical process for the growth of EBVs and the associated tumors. The present invention also provides method of treating and imaging EBV-associated cancers.本發明提供一種細胞核穿透性小分子抑制劑L2P4(其中L2為4-(4-(二乙基氨基)苯乙烯基)-N-羧甲基吡啶陽離子氯化物且P4是一段含有CAhxYFMVFGGRrRK的氨基酸序列,此二者透過醯胺鍵結合)以及此抑制劑的合成,它以EBVs及相關腫瘤的生長之必要程序的EBNA1的二聚合中的二聚界面為標靶從而達到對EBV陽性細胞及腫瘤的有效抑制。本發明亦提供對EBV相關癌症的治療和成像的方法。
