靶向β-葡萄糖醛酸苷酶的抗肿瘤药物研究进展  

Research Process of Selective Anti-Tumor Drugs Targeting β-glucuronidase

作　　者：郭家鼎 郝佳[1] GUO Jiading;HAO Jia(Tianjin University of Traditional Chinese Medicine,Tianjin Key Laboratory of TCM Chemistry and Analysis,Tianjin 300193,China)

机构地区：[1]天津中医药大学,天津市中药化学与分析重点实验室,天津300193

出　　处：《天津科技》2018年第4期62-66,共5页Tianjin Science & Technology

基　　金：天津市应用基础与前沿技术研究计划(一般项目)15JCYBJC29300

摘　　要：β-葡萄糖醛酸苷酶(β-Glucuronidase,简称βGU)是参与机体多种代谢过程的重要酸性水解酶。βGU具有极高的催化效率,几乎可以水解任何含β-葡萄糖醛酸苷结构的底物。其活性与pH值相关,在酸性环境下(pH值为4左右)活性最佳。由于该酶在广泛种类的恶性肿瘤中高度表达,及肿瘤酸性微环境对其活性的催化作用,因而在靶向性抗肿瘤药物的研究与开发中成为新的研究热点。综述了β-葡萄糖醛酸苷酶与肿瘤的关系以及基于β-葡萄糖醛酸苷酶的抗肿瘤药物的研发近况。β-Glucuronidase(βGU)is an acidic lysosomal enzyme,which plays a key role in various metabolic processes of the body.In consideration of the increased activity ofβGU in tumour tissue as opposed to normal tissue due to the increased expression of the enzyme and the acidic tumor microenvironment,βGU has become a novel research hotspot in the research and development of selective anti-tumor drugs.This review summarizes the relationship betweenβGU and tumor and the major progresses that have been reported in recent years.

关 键 词：β-葡萄糖醛酸苷酶(βGU) 靶向性抗肿瘤药物 前药设计 

分 类 号：R979.1[医药卫生—药品]