A platform for efficient, thiol-stable conjugation to albumin's native single accessible cysteineElectronic supplementary information (ESI) available: LC-MS, ES-MS and deconvoluted spectra for all reactions with proteins described herein, and 1H and 13C NMR spectra for all small molecule constructs. See DOI: 10.1039/c5ob01205h

Herein we report the use of bromomaleimides for the construction of stable albumin conjugates via conjugation to its native, single accessible, cysteine followed by hydrolysis. Advantages over the classical maleimide approach are highlighted in terms of quantitative hydrolysis and absence of undesir...

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Main Authors: Smith, Mark E. B, Caspersen, Mikael B, Robinson, Eifion, Morais, Maurício, Maruani, Antoine, Nunes, João P. M, Nicholls, Karl, Saxton, Malcolm J, Caddick, Stephen, Baker, James R, Chudasama, Vijay
Format: Article
Language:English
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Summary:Herein we report the use of bromomaleimides for the construction of stable albumin conjugates via conjugation to its native, single accessible, cysteine followed by hydrolysis. Advantages over the classical maleimide approach are highlighted in terms of quantitative hydrolysis and absence of undesirable retro-Michael deconjugation. Thiol-stable albumin biologics are enabled by controlled, quantitative hydrolysis of maleimide-albumin conjugates, i.e. with no retro-Michael.
ISSN:1477-0520
1477-0539
DOI:10.1039/c5ob01205h