摘要
基于肿瘤细胞与正常细胞葡萄糖代谢差异的肿瘤沃伯格效应,是目前新型靶向抗肿瘤药物开发的研究热点之一。本文以沃伯格效应的代谢特征和特异性生物标识物为出发点,从靶向葡萄糖转运蛋白(GLUTs)生物靶点和利用肿瘤葡萄糖代谢亢进的生物特征这两个层面,综述了具有代表性的GLUTs抑制剂以及GLUTs靶向型糖偶联抗肿瘤药物的研发现状,讨论并解析通过靶向沃伯格效应开发抗肿瘤药物的设计思路、实施策略与推广前景。
Increased glycolysis in malignant tumors has been one of the hallmarks and biotargets of tumor targeting that enable the design and development of novel targeted therapy agents.In this review,by focusing on the Warburg effect-targeted drug discovery and the unique concepts for development of glucose transporters(GLUTs)-targeted anticancer agents,we examine the current scenario with a brief introduction of anticancer GLUTs inhibitors and glycoconjugated antitumor examples,to provide an overview of studies of the Warburg effect-targeted anticancer drug development,the design strategy and useful perspectives for new-generation of targeted chemotherapeutic agents.
作者
孙子茹
刘胜男
高清志
Ziru Sun;Shengnan Liu;Qingzhi Gao(School of Pharmaceutical Science and Technology,Tianjin Key Laboratory for Modern Drug Delivery&High-Efficiency,Tianjin University,Tianjin 300072,China;Institute of Molecular Plus,Tianjin University,Tianjin 300072,China)
出处
《化学进展》
SCIE
CAS
CSCD
北大核心
2020年第12期1869-1878,共10页
Progress in Chemistry
基金
国家自然科学基金项目(No.21772144)资助。
关键词
沃伯格效应
葡萄糖转运蛋白
靶向抗肿瘤
糖偶联抗肿瘤药物
Warburg effect
glucose transporters
targeted anti-cancer therapy
glycoconjugated anticancer agents
作者简介
Corresponding author:刘胜男,e-mail:shengnan_liu@tju.edu.cn;Corresponding author:高清志,e-mail:qingzhi@tju.edu.cn。
