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Optimisation of the dibromomaleimide (DBM) platform for native antibody conjugation by accelerated post-conjugation hydrolysis

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Abstract

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.

Graphical abstract: Optimisation of the dibromomaleimide (DBM) platform for native antibody conjugation by accelerated post-conjugation hydrolysis

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Publication details

The article was received on 27 Jan 2017, accepted on 03 Mar 2017, published on 14 Mar 2017 and first published online on 14 Mar 2017


Article type: Paper
DOI: 10.1039/C7OB00220C
Citation: Org. Biomol. Chem., 2017, Advance Article
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    Optimisation of the dibromomaleimide (DBM) platform for native antibody conjugation by accelerated post-conjugation hydrolysis

    M. Morais, J. P. M. Nunes, K. Karu, N. Forte, I. Benni, M. E. B. Smith, S. Caddick, V. Chudasama and J. R. Baker, Org. Biomol. Chem., 2017, Advance Article , DOI: 10.1039/C7OB00220C

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