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Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
Antibody Conjugations via Glycosyl Remodeling
Hanna Toftevall1, Helén Nyhlén1, Fredrik Olsson1
1Genovis AB, Lund, Sweden.
Abstract:
The antibody Fc-glycans are interesting targets for conjugation of cytotoxic compounds due to their localization and their chemical composition. In striving to obtain site-specific conjugates, the antibody Fc-glycans have been explored in numerous ways. Here we present a two-step enzymatic methodology coupled to click-chemistry for conjugation at the core GlcNAc of the Fc-glycan resulting in ADCs that are homogenous with a DAR 2.0, retain antigen binding, and display cytotoxic anti-tumor effects both in vitro and in vivo.
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