The success of recent antibody conjugates with high drug loading in anticancer therapy has spurred interest in synthetic strategies for high and defined degrees of drug-to-antibody ratios (DARs). Here we describe a glycoengineering methodology that combines highly selective galactosylation with oxidation to generate aldehyde groups that can be used in bioorthogonal conjugation reactions, such as a tandem Knoevenagel-Michael additions.  Key enzymes in these transformations are glycosyltransferases and oxidases. This approach offers a selective route to conjugates from native antibodies with high drug loading and thus illustrates how biocatalysis can be used for the generation of biopharmaceuticals from native proteins using mild reaction conditions.

Application of carbohydrate-active enzymes for bioconjugation

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