位点专一的抗体-药物偶联物的研究进展  

Advances in the study of site-specific antibody-drug conjugates

作　　者：孙玉[1,2] 黄蓉[1] 孙柏旺[1] 

机构地区：[1]东南大学化学化工学院,江苏南京211189 [2]皖南医学院药学院,安徽芜湖241002

出　　处：《药学学报》2015年第10期1225-1231,共7页Acta Pharmaceutica Sinica

基　　金：国家国际科技合作专项资助项目(2015DFG42240);国家自然科学基金资助项目(21371031);皖南医学院重点科研项目培育基金资助项目(WK2014Z06)

摘　　要：抗体-药物偶联物是一类能有效提高传统抗肿瘤药物疗效的靶向制剂。但传统偶联方式无法控制药物和抗体偶联的位置和数目,所合成的抗体-药物偶联物结构不均一,批次可重复性差,治疗指数低。新型定点偶联技术可以有效控制药物结合的位置,获得药抗比均一的偶联物。本文总结了抗体-药物偶联物的发展过程,重点介绍了位点专一的抗体-药物偶联物的研究现状和定点偶联技术。Antibody drug conjugates （ADCs） are an emerging class of targeted therapeutics with the potential to improve therapeutic index over the traditional chemotherapy. However, it is difficult to control the site and stoichiometry of conjugation in mAb, typically resulting in heterogeneous mixtures of ADCs that are difficult to optimize. New methods for site-specific drug attachment allow development of more homogeneous conjugates and control of the site of drug attachment. In this article, the new literature on development of ADCs and site-specific ADCs is reviewed. In addition, we summarized the various strategies in production of site-specific ADCs.

关 键 词：定点偶联 抗体-药物偶联物 癌症靶向治疗 

分 类 号：R916[医药卫生—药学]