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Issue 17, 2019
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New linker structures applied in glycosite-specific antibody drug conjugates

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Abstract

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.

Graphical abstract: New linker structures applied in glycosite-specific antibody drug conjugates

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Publication details

The article was received on 15 May 2019, accepted on 14 Jul 2019 and first published on 15 Jul 2019


Article type: Research Article
DOI: 10.1039/C9QO00646J
Org. Chem. Front., 2019,6, 3144-3149

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    New linker structures applied in glycosite-specific antibody drug conjugates

    Faridoon, W. Shi, K. Qin, Y. Tang, M. Li, D. Guan, X. Tian, B. Jiang, J. Dong, F. Tang and W. Huang, Org. Chem. Front., 2019, 6, 3144
    DOI: 10.1039/C9QO00646J

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