前药在靶向抗肿瘤药物研究中的应用进展  

Application Progress of Prodrug for the Research of the Targeted Antitumor Drugs

作　　者：汪柱勇 陈亚军[1] 张子健 吴健龙 闵真立[1] WANG Zhuyong;CHEN Yajun;ZHANG Zijian;WU Jianlong;MIN Zhenli(College of Medical,Wuhan University of Science and Technology,Wuhan 430040,China)

机构地区：[1]武汉科技大学医学院,武汉430040

出　　处：《中国现代应用药学》2021年第18期2323-2332,共10页Chinese Journal of Modern Applied Pharmacy

摘　　要：前药原理是一个经典的药物化学理论,近年来,随着人们对肿瘤形成机制认识的深入,这一原理在抗肿瘤药物研究中有了新的应用。人们可以利用肿瘤细胞与正常细胞在细胞微环境、特定的酶以及特异性表面抗原方面的差异来设计前药,从而实现母药的靶向性,减少不良反应,同时也可能改善母药的溶解性、生物利用度或者扩大母药的治疗窗口等。本文对近年来应用于抗肿瘤领域的靶向抗肿瘤前药发展情况进行了综述。The principle of prodrug is classical in medicinal chemistry, which has been applied newly in researches on targeted antitumor drugs as the mechanisms of tumors were continually revealed in recent years. The prodrugs can be designed to improve water solubility and bioavailability or broaden the therapeutic window of parent drugs according to the differences between a normal cell and a tumor cell, such as cell microenvironment, the special enzymes and surface antigens. This article mainly reviews the advances on the application of prodrug in the research of the targeted antitumor drugs in recent years.

关 键 词：靶向抗肿瘤药物 前药 微环境 酶 抗体偶联药物 

分 类 号：R914[医药卫生—药物化学]