auristatin类细胞毒素及其在抗体药物偶联物中的应用  

Auristatin cytotoxins and their application in antibody-drug conjugate

作　　者：范啸宇 高文龙 杜子秀(综述)[1] Fan Xiaoyu;Gao Wenlong;Du Zixiu(School of Pharmacy,Shanghai Jiaotong University,Shanghai 200240,China)

机构地区：[1]上海交通大学药学院,200240

出　　处：《国际生物制品学杂志》2018年第5期253-257,共5页International Journal of Biologicals

摘　　要：auristatin类细胞毒素作为抗体药物偶联物（antibody-drug conjugate，ADC）的主要成分，因具有高度生物活性而引起学术界和产业界的广泛关注。研究发现，对auristatin类细胞毒素结构进行修饰和优化，可以获得效果更好的生物活性药物。此文介绍了auristatin类细胞毒素及其在ADC中的应用研究，概述了部分auristatin类ADC的临床开发现状。Due to its high biological activity, auristatin cytotoxin, as a main component in antibody-drug conjugate （ADC）, has attracted wide attention from academia and industry. Studies have shown that more efficient biologically active drugs can be developed by modifying and optimizing the structures of auristatin cytotoxins. This review introduces the auristatin cytotoxins and their application in ADCs, and outlines the clinical research status of some auristatin-based ADCs.

关 键 词：免疫毒素类 抗体 单克隆 免疫轭合物 抗肿瘤药 

分 类 号：R392[医药卫生—免疫学]