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Enabling the controlled assembly of antibody conjugates with a loading of two modules without antibody engineering

“…only such a result could have yielded the observed SDS-PAGE profile and PDAR. Despite the challenges of using mass spec for characterisation of antibody conjugates, 16 especially for disulfide modified conjugates, 13 we obtained mass spec data for conjugate 7 (see ESI for details † ), which further verified our observation; i.e. we observed two additions of bis-diBrPD 1 to Herceptin™ (see representation in Fig.…”

“… 10 The dibromomaleimide platform has also been shown to be effective in vivo by Jackson and co-workers. 13 Whilst this approach, as well as others, 10 , 13 , 14 offer advances in terms of providing homogeneous DAR 4 conjugates starting from a non-engineered antibody scaffold, there has as yet been no translation of the technologies to form controlled DAR 2 conjugates. Nonetheless, we set out to explore if we could exploit the efficient functional re-bridging of disulfides with diBrPDs as a conduit to realise the goal of controlled DAR 2 conjugate formation starting from a native antibody scaffold.…”