title: Optimisation of the dibromomaleimide (DBM) platform for native antibody conjugation by accelerated post-conjugation hydrolysis.
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.
authors.affiliation: Department of Chemistry, UCL, 20 Gordon St, London, UK WC1H 0AJ. j.r.baker@ucl.ac.uk v.chudasama@ucl.ac.uk.
authors.forename: Maurício
authors.identifier: http://orcid.org/0000-0001-7718-1629
authors.initials: M
authors.lastname: Morais
authors.affiliation: Department of Chemistry, UCL, 20 Gordon St, London, UK WC1H 0AJ. j.r.baker@ucl.ac.uk v.chudasama@ucl.ac.uk.
authors.forename: João P M
authors.initials: JPM
authors.lastname: Nunes
authors.affiliation: Department of Chemistry, UCL, 20 Gordon St, London, UK WC1H 0AJ. j.r.baker@ucl.ac.uk v.chudasama@ucl.ac.uk.
authors.forename: Kersti
authors.initials: K
authors.lastname: Karu
authors.affiliation: Department of Chemistry, UCL, 20 Gordon St, London, UK WC1H 0AJ. j.r.baker@ucl.ac.uk v.chudasama@ucl.ac.uk.
authors.forename: Nafsika
authors.initials: N
authors.lastname: Forte
authors.affiliation: Department of Chemistry, UCL, 20 Gordon St, London, UK WC1H 0AJ. j.r.baker@ucl.ac.uk v.chudasama@ucl.ac.uk.
authors.forename: Irene
authors.initials: I
authors.lastname: Benni
authors.affiliation: Department of Chemistry, UCL, 20 Gordon St, London, UK WC1H 0AJ. j.r.baker@ucl.ac.uk v.chudasama@ucl.ac.uk.
authors.forename: Mark E B
authors.initials: MEB
authors.lastname: Smith
authors.affiliation: Department of Chemistry, UCL, 20 Gordon St, London, UK WC1H 0AJ. j.r.baker@ucl.ac.uk v.chudasama@ucl.ac.uk.
authors.forename: Stephen
authors.initials: S
authors.lastname: Caddick
authors.affiliation: Department of Chemistry, UCL, 20 Gordon St, London, UK WC1H 0AJ. j.r.baker@ucl.ac.uk v.chudasama@ucl.ac.uk.
authors.forename: Vijay
authors.identifier: http://orcid.org/0000-0002-8876-3285
authors.initials: V
authors.lastname: Chudasama
authors.affiliation: Department of Chemistry, UCL, 20 Gordon St, London, UK WC1H 0AJ. j.r.baker@ucl.ac.uk v.chudasama@ucl.ac.uk.
authors.forename: James R
authors.identifier: http://orcid.org/0000-0002-7223-2279
authors.initials: JR
authors.lastname: Baker