The availability of tools to generate homogeneous and stable antibody conjugates without recombinant DNA technology is a valuable asset in fields spanning from diagnostics to imaging and therapeutics. We present here a general approach for the conjugation to human IgG1 antibodies, by employing a straightforward two-stage protocol based on antibody deglycosylation followed by tyrosinase-mediated -quinone strain-promoted click chemistry. The technology is validated by the efficient and clean generation of highly potent DAR2 and DAR4 antibody-drug conjugates (ADCs) with cytotoxic payloads MMAE or PBD dimer, and their evaluation.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8532111 | PMC |
| http://dx.doi.org/10.1021/acs.bioconjchem.1c00351 | DOI Listing |
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