A platform for efficient, thiol-stable conjugation to albumin's native single accessible cysteine

Mark E. B. Smith; Mikael B. Caspersen; Eifion Robinson; Maurício Morais; Antoine Maruani; João P. M. Nunes; Karl Nicholls; Malcolm J. Saxton; Stephen Caddick; James R. Baker; Vijay Chudasama

doi:10.1039/C5OB01205H

A platform for efficient, thiol-stable conjugation to albumin's native single accessible cysteine†

Mark E. B. Smith,^a Mikael B. Caspersen,^b Eifion Robinson,^a Maurício Morais,^a Antoine Maruani,^a João P. M. Nunes,^a Karl Nicholls,^b Malcolm J. Saxton,^b Stephen Caddick,^a James R. Baker*^a and Vijay Chudasama*^a

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^a Department of Chemistry, University College London, London, UK
E-mail: j.r.baker@ucl.ac.uk, v.chudasama@ucl.ac.uk
Tel: +44 (0)20 7679 2653, +44 (0)20 7679 2077

^b Novozymes Biopharma UK Ltd, Castle Court, 59 Castle Boulevard, Nottingham, UK

Abstract

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.

Organic & Biomolecular Chemistry

A platform for efficient, thiol-stable conjugation to albumin's native single accessible cysteine†

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A platform for efficient, thiol-stable conjugation to albumin's native single accessible cysteine

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