Site-selective lysine conjugation methods and applications towards antibody-drug conjugates.
Site-selective lysine conjugation methods and applications towards antibody-drug conjugates.
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DOI：
10.1039/d1cc03976h
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发表时间：
2021-10-14
期刊：
影响因子：
--
通讯作者：
Baker JR
中科院分区：
文献类型：
--
作者：
Haque M;Forte N;Baker JR
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. In this feature article we discuss developments in site-selective lysine modification methodologies and their application towards the synthesis of antibody–drug conjugates; including our recent work on a cysteine-to-lysine transfer (CLT) protocol.
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