Site-selective template-directed synthesis of antibody Fc conjugates with concomitant ligand release
Viktoriia Postupalenko, Léo Marx, Mathilde Pantin, David Viertl, Nadège Gsponer, Gaëlle Giudice, Natalia Gasilova, Margret Schottelius, Frédéric Lévy, Patrick Garrouste, Jean‐Manuel Segura, Origène Nyanguile
Abstract
A one step template-directed method for site-specific conjugation of payloads to monoclonal antibodies is reported. Near 100% modification at a single lysine residue of the antibody Fc domain is achieved with a drug to antibody ratio of 2.
Topics & Concepts
ConjugateChemistryMonoclonal antibodyPeptideCombinatorial chemistryLigand (biochemistry)ReagentAtezolizumabCarbodiimideChelationStereochemistryAntibodyBiochemistryReceptorImmunotherapyImmune systemOrganic chemistryBiologyImmunologyMathematical analysisPembrolizumabMathematicsMonoclonal and Polyclonal Antibodies ResearchRadiopharmaceutical Chemistry and ApplicationsHER2/EGFR in Cancer Research