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Optimised approach to albumin–drug conjugates using monobromomaleimide-C-2 linkers

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Abstract

Conjugation of therapeutics to human serum albumin (HSA) using bromomaleimides represents a promising platform for half-life extension. We show here that the Cys-34 crevice substantially reduces the rate of serum stabilising maleimide hydrolysis in these conjugates, necessitating reagent optimisation. This improved reagent design is applied to the construction of an HSA-paclitaxel conjugate, preventing drug loss during maleimide hydrolysis.

Graphical abstract: Optimised approach to albumin–drug conjugates using monobromomaleimide-C-2 linkers

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Publication details

The article was received on 29 Mar 2019, accepted on 25 Jul 2019 and first published on 14 Aug 2019


Article type: Communication
DOI: 10.1039/C9OB00721K
Org. Biomol. Chem., 2019, Advance Article
  • Open access: Creative Commons BY-NC license
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    Optimised approach to albumin–drug conjugates using monobromomaleimide-C-2 linkers

    A. Wall, K. Nicholls, M. B. Caspersen, S. Skrivergaard, K. A. Howard, K. Karu, V. Chudasama and J. R. Baker, Org. Biomol. Chem., 2019, Advance Article , DOI: 10.1039/C9OB00721K

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