Improvement of Antibody Activity by Controlling Its Dynamics Using the Glycan–Lectin Interaction

Antibody dynamics on membranes, such as endocytosis and clustering, are vital in determining antibody functions. In this study, we demonstrated that glycan conjugation can modulate antibody dynamics through the glycan–lectin interaction to regulate its potency. The anti‐HER2 antibody, an anti‐breast‐cancer antibody, was conjugated with galactose‐containing N‐glycan, and its internalization was suppressed by interaction with galectin‐3, leading to enhanced complement‐dependent cytotoxic (CDC) activity. This glycan–antibody conjugate is proposed as a new approach to modulate antibody activity and may provide an alternative strategy for redeveloping antibody drugs that do not exhibit sufficient activity. The anti‐HER2 antibody was conjugated with galactose‐containing N‐glycan, and its internalization was suppressed by the interaction with galectin‐3, leading to the enhancement of complement‐dependent cytotoxic (CDC) activity. The glycan–antibody conjugate suggests a new approach to modulate antibody activity and might provide an alternative strategy for enhancing antibody activity.