title: Protocols for lysine conjugation.
abstract: 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.
authors.affiliation: Natural Product and Protein Chemistry, Sanofi, Vitry-sur-Seine, France.
authors.forename: Marie-Priscille
authors.initials: MP
authors.lastname: Brun
authors.forename: Laurence
authors.initials: L
authors.lastname: Gauzy-Lazo
mesh_terms: D018796:Immunoconjugates / Q000737:chemistry*; D007202:Indicators and Reagents / Q000737:chemistry; D007460:Iodoacetamide / Q000737:chemistry; D008239:Lysine / Q000737:chemistry*; D008301:Maleimides / Q000737:chemistry; D011725:Pyridines / Q000737:chemistry; D013388:Succinimides / Q000737:chemistry
chemical_list: D018796:Immunoconjugates; D007202:Indicators and Reagents; D008301:Maleimides; D011725:Pyridines; D013388:Succinimides; C032620:succinimide; C043592:maleimide; C035119:methyl 2-pyridyl disulfide; D008239:Lysine; D007460:Iodoacetamide