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New linker structures applied in glycosite-specific antibody drug conjugates

文献类型：期刊论文

作者Faridoon2; Shi, Wei1,2; Qin, Ken1,2; Tang, Yubo2,3; Li, Mingjie2,3; Guan, Dongliang1,2; Tian, Xiaobo2; Jiang, Bofeng2; Dong, Jinhua3; Tang, Feng1,2
刊名ORGANIC CHEMISTRY FRONTIERS
出版日期2019-09-07
卷号6期号:17页码:3144-3149
ISSN号2052-4129
DOI10.1039/c9qo00646j
通讯作者Tang, Feng(tangfeng2013@simm.ac.cn) ; Huang, Wei(huangwei@simm.ac.cn)
英文摘要Glycosite-specific antibody drug conjugates (ADCs) allow selective conjugation of a small-molecule payload onto the conserved N-glycan of Asn297 of antibody Fc domains, and lead to a highly homogeneous structure in specific conjugation site and fixed drug-to-antibody ratio (DAR), which are crucial for pharmacokinetics, pharmacodynamics and efficacy of the ADCs. The limited structural diversity of linkers in glycosite-specific ADCs is due to the scarcity of efficient chemistry for IgG glycan conjugation. Herein we describe two new linkers, 2-aminobenzamidoxime and mercaptoethylpyrazolone, which rapidly, efficiently and selectively react with aldehyde-tagged N-glycan after IgG glycoengineering. The constructed novel glycosite-specific ADCs demonstrated excellent anti-tumor cytotoxicity and fluorescence properties or enhanced stability.
WOS关键词SITE-SPECIFIC CONJUGATION ; IGG ANTIBODIES ; GLYCOSYLATION ; PROTEINS
资助项目National Natural Science Foundation of China (NNSFC)[21572244] ; National Natural Science Foundation of China (NNSFC)[21877116] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program of China[2018ZX09711002-006] ; China Postdoctoral Science Foundation Postdoctoral Innovative Talent Support Program[BX20180339]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000483840200012
出版者ROYAL SOC CHEMISTRY
源URL[http://119.78.100.183/handle/2S10ELR8/288796]  
专题中国科学院上海药物研究所
通讯作者Tang, Feng; Huang, Wei
作者单位1.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
2.Chinese Acad Sci, CAS Key Lab Receptor Res, CAS Ctr Excellence Mol Cell Sci, Ctr Biotherapeut Discovery Res,Shanghai Inst Mat, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
3.Shenyang Pharmaceut Univ, Minist Educ, Key Lab Struct Based Drug Design & Discovery, Shenyang 110016, Liaoning, Peoples R China
推荐引用方式
GB/T 7714		 Faridoon,Shi, Wei,Qin, Ken,et al. New linker structures applied in glycosite-specific antibody drug conjugates[J]. ORGANIC CHEMISTRY FRONTIERS,2019,6(17):3144-3149.
APA Faridoon.,Shi, Wei.,Qin, Ken.,Tang, Yubo.,Li, Mingjie.,...&Huang, Wei.(2019).New linker structures applied in glycosite-specific antibody drug conjugates.ORGANIC CHEMISTRY FRONTIERS,6(17),3144-3149.
MLA Faridoon,et al."New linker structures applied in glycosite-specific antibody drug conjugates".ORGANIC CHEMISTRY FRONTIERS 6.17(2019):3144-3149.

入库方式： OAI收割

来源：上海药物研究所

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