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.
Preview |
Text
Baker_Optimised approach to albumin-drug conjugates using monobromomaleimide-C-2 linkers_VoR.pdf Download (1MB) | Preview |
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 |
Archive Staff Only
 |
View Item |
