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Data for Covalent cell surface recruitment of chemotherapeutic polymers enhances selectivity and activity
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Tomás, Ruben M. F. and Gibson, Matthew I. (2021) Data for Covalent cell surface recruitment of chemotherapeutic polymers enhances selectivity and activity. [Dataset]
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Official URL: http://wrap.warwick.ac.uk/156965/
Abstract
Synthetic macromolecular chemotherapeutics inspired by host defence peptides can disrupt cell membranes and are emerging as agents for the treatment of cancer and infections. However, their off-target effects remain a major unmet challenge. Here we introduce a covalent recruitment strategy, whereby metabolic oligosaccharide engineering is used to label targeted cells with azido glycans, to subsequently capture chemotherapeutic polymers by a bio-orthogonal click reaction. This results in up to 10-fold reduction in EC50 and widening of the therapeutic window. Cell death is induced by not only membrane leakage, but also by apoptosis due to the conjugated chemotherapeutic being internalised by glycan recycling. Covalent recruitment also lead to increased penetration and significant cell death in a 3-D tumour model in just 3 hours, whereas doxorubicin required 24 hours. This conceptual approach of ‘engineering cells to capture polymers’ rather than ‘engineering polymers to target cells’ will bring new opportunities in non-traditional macromolecular therapeutics.
Item Type: | Dataset | |||||||||
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Subjects: | Q Science > QH Natural history Q Science > QP Physiology Q Science > QR Microbiology R Medicine > RS Pharmacy and materia medica |
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Divisions: | Faculty of Science, Engineering and Medicine > Science > Chemistry | |||||||||
Library of Congress Subject Headings (LCSH): | Drug resistance in cancer cells, Oligosaccharides, Cell membranes, Peptide antibiotics | |||||||||
Publisher: | University of Warwick, Department of Chemistry | |||||||||
Official Date: | 19 August 2021 | |||||||||
Dates: |
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Status: | Not Peer Reviewed | |||||||||
Publication Status: | Published | |||||||||
Media of Output (format): | .xlsx | |||||||||
Access rights to Published version: | Open Access (Creative Commons) | |||||||||
Copyright Holders: | University of Warwick | |||||||||
Description: | Tabulated data underpinning the manuscript Data is organised according to each figure in the main paper and supporting information and the heading and legend of each figure can be used to understand the contents. All headings are explained in the individual tabs of the worksheet |
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Date of first compliant deposit: | 19 August 2021 | |||||||||
Date of first compliant Open Access: | 19 August 2021 | |||||||||
RIOXX Funder/Project Grant: |
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Contributors: |
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