Protocols for Lysine Conjugation

Currently, the most widely used chemical methodology for the conjugation of drugs to monoclonal antibodies involves either lysine or cysteine residues. In this chapter, several methods for the preparation of antibody–drug conjugates (ADCs) through conjugation of drugs to solvent-exposed ε-amino groups of lysine residues are described. These methods apply to various cytotoxic agents, both tubulin binders and DNA-targeting agents and different types of linkers, cleavable or not, peptidic or disulfide-based, for example.