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Morais, Maurício; Nunes, João P M; Karu, Kersti; Forte, Nafsika; Benni, Irene; Smith, Mark E B; Caddick, Stephen; Chudasama, Vijay; Baker, James R
Organic & biomolecular chemistry, 2017-Apr-05, Volume: 15, Issue: 14Journal Article
Disulfide bridging offers a convenient approach to generate site-selective antibody conjugates from native antibodies. To optimise the reagents available to achieve this strategy, we describe here the use of dibromomaleimides designed to undergo accelerated post-conjugation hydrolysis. Conjugation and hydrolysis, which serve to 'lock' the conjugates as robustly stable maleamic acids, is achieved in just over 1 h. This dramatic acceleration is also shown to infer significant improvements in homogeneity, as demonstrated by mass spectrometry analysis.
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