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

Wall, A; Nicholls, K; Caspersen, MB; Skrivergaard, S; Howard, KA; Karu, K; Chudasama, V; (2019) Optimised approach to albumin-drug conjugates using monobromomaleimide-C-2 linkers. Organic & Biomolecular Chemistry , 17 (34) pp. 7870-7873. 10.1039/c9ob00721k. Green open access

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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.

Type: Article
Title: Optimised approach to albumin-drug conjugates using monobromomaleimide-C-2 linkers
Location: England
Open access status: An open access version is available from UCL Discovery
DOI: 10.1039/c9ob00721k
Publisher version: https://doi.org/10.1039/c9ob00721k
Language: English
Additional information: © The Royal Society of Chemistry 2019. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence (https://creativecommons.org/licenses/by/3.0/).
UCL classification: UCL
UCL > Provost and Vice Provost Offices > UCL BEAMS
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/10080435
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