Peroxide-cleavable linkers for antibody–drug conjugates

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Authors

Nicola Ashman · University of Cambridge

Jonathan D. Bargh · University of Cambridge

Stephen J. Walsh · University of Cambridge

Ryan Greenwood · AstraZeneca (United Kingdom)

Arnaud Tiberghien · Spirogen (United Kingdom)

Jason S. Carroll · Cancer Research UK

David R. Spring ·

Abstract

Antibody-drug conjugates containing peroxide-cleavable arylboronic acid linkers are described, which target the high levels of reactive oxygen species (ROS) in cancer. The arylboronic acid linkers rapidly release a payload in the presence of hydrogen peroxide, but remain stable in plasma. Anti-HER2 and PD-L1 peroxide-cleavable ADCs exhibited potent cytotoxicity <i>in vitro</i>.

Topics & Keywords

HER2/EGFR in Cancer Research Monoclonal and Polyclonal Antibodies Research Radiopharmaceutical Chemistry and Applications

Publication Details

Published in: Chemical Communications

Volume 59, Issue 13, pp. 1841-1844

DOI: 10.1039/d2cc06677g

Field-Weighted Citation Impact: 5.29

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Peroxide-cleavable linkers for antibody–drug conjugates

Authors

Abstract

Topics & Keywords

Publication Details