Optimisation of the dibromomaleimide (DBM) platform for native antibody conjugation by accelerated post-conjugation hydrolysisElectronic supplementary information (ESI) available. See DOI: 10.1039/c7ob00220c

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 a...

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Main Authors: Morais, Maurício, Nunes, João P. M, Karu, Kersti, Forte, Nafsika, Benni, Irene, Smith, Mark E. B, Caddick, Stephen, Chudasama, Vijay, Baker, James R
Format: Article
Language:English
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Summary: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. Dibromomaleimide (DBM) reagents are described which hydrolyse rapidly post-conjugation, representing an optimised platform for homogeneous and stable antibody conjugation.
ISSN:1477-0520
1477-0539
DOI:10.1039/c7ob00220c