摘要
T-LAK细胞源蛋白激酶(TOPK)/PDZ结合的蛋白激酶(PBK)在正常的人体组织中呈低表达或不表达,而在多种恶性肿瘤存在过量表达的现象,机制是通过参与介导细胞内的多条信号通路和影响多种细胞因子,调控肿瘤细胞的增殖、侵袭和转移,甚至能调节肿瘤细胞抵抗凋亡。目前已知的具有TOPK抑制活性的化合物来源广泛,有研究人员针对TOPK的结构而设计并合成化合物,从已经运用于临床多年的后来被发现有TOPK抑制活性药物,还有从植物中直接提取的。因为TOPK抑制剂在肿瘤治疗中有很大的应用前景,本文将综述TOPK肿瘤学研究进展,并总结其抑制剂的研发现状。
T-LAK cell-originated protein kinase（ TOPK）/PDZ-binding kinase（ PBK） is little or not expressed in the normal tissues,but highly in many kinds of tumor cells. TOPK is involved in regulating the proliferation,invasion and metastasis of tumor cells and even regulating the resistance of tumor cells to apoptosis by mediating the multiple signaling pathways and affecting a variety of cytokines. The currently known compounds with TOPK inhibitory activity are widely available. Some were developed by the structure of TOPK. Some used for other diseases years were found to have TOPK inhibitory activity. Some were extracted from plants. This review mainly focuses on the development of TOPK and its inhibitors in oncology.
作者
孙宇通
宋树勇
杨宜球
汪桂飞
谢晓阳
黄云生
SUN Yu-tong;SONG Shu-yong;YANG Yi-qiu;WANG Gui-fei;XIE Xiao-yang;HUANG Yun-sheng(School of Pharmacy, Guangdong Medical University, Dongguan 523808, Chin)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2018年第13期1502-1509,共8页
Chinese Journal of New Drugs
基金
广东省自然科学基金资助项目(2016A030313676)
