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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.


Marie-Priscille Brun, Laurence Gauzy-Lazo. Protocols for lysine conjugation. Methods in molecular biology (Clifton, N.J.). 2013;1045:173-87

PMID: 23913147

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