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Issue 34, 2019
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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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Supplementary files

Article information


Submitted
29 Mar 2019
Accepted
25 Jul 2019
First published
14 Aug 2019

This article is Open Access

Org. Biomol. Chem., 2019,17, 7870-7873
Article type
Communication

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, 17, 7870
DOI: 10.1039/C9OB00721K

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