抗体
同种类的
化学
聚糖
药品
结合
生物化学
组合化学
立体化学
计算生物学
糖蛋白
药理学
生物
数学分析
免疫学
数学
物理
热力学
作者
Xiao Zhang,Chong Ou,Huiying Liu,Sunaina Kiran Prabhu,Chao Li,Qiang Yang,Lai‐Xi Wang
标识
DOI:10.1021/acschembio.1c00597
摘要
of serotype M49 (Endo-S2) exhibited remarkable activity in transferring the functionalized disaccharides carrying site-selectively modified azide, biotin, or fluorescent tags to antibodies without hydrolyzing the resulting transglycosylation products. This discovery, together with the excellent Fc deglycosylation activity of Endo-S2 on recombinant antibodies, allowed direct labeling and functionalization of antibodies in a one-pot manner without the need of intermediate and enzyme separation. The site-specific introduction of varied numbers of azide groups enabled a highly efficient synthesis of homogeneous antibody-drug conjugates (ADCs) with a precise control of the drug-to-antibody ratio (DAR) ranging from 2 to 12 via a copper-free strain-promoted click reaction. Cell viability assays showed that ADCs with higher DARs were more potent in killing antigen-overexpressed cells than the ADCs with lower DARs. This new method is expected to find applications not only for antibody-drug conjugation but also for cell labeling, imaging, and diagnosis.
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