%O This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
%C England
%X Site-selective protein modification is of significant interest in chemical biology research, with lysine residues representing a particularly challenging target. Whilst lysines are popular for bioconjugation, due to their nucleophilicity, solvent accessibility and the stability of the resultant conjugates, their high abundance means site-selectivity is very difficult to achieve. Antibody-drug conjugates (ADCs) present a powerful therapeutic application of protein modification, and have often relied extensively upon lysine bioconjugation for their synthesis. Here we discuss advances in methodologies for achieving site-selective lysine modification, particularly within the context of antibody conjugate construction, including the cysteine-to-lysine transfer (CLT) protocol which we have recently reported.
%J Chemical Communications
%L discovery10135863
%D 2021
%T Site-selective lysine conjugation methods and applications towards antibody-drug conjugates
%A M Haque
%A N Forte
%A JR Baker