Towards a glutathione-cleavable azobenzene linker for antibody–drug conjugates
Herein we describe the development of a novel azobenzene-containing glutathione-cleavable linker for use in antibody-drug conjugates (ADCs). This linker demonstrated efficient payload release under elevated glutathione levels while maintaining stability in human plasma. An anti-HER2 ADC incorporating this linker exhibited potent <i>in vitro</i> cytotoxicity and selective activity towards HER2-positive cell lines.
Authors
- Roshan Patel (ORCID: https://orcid.org/0000-0001-8498-0189)
- Mia Kapun (ORCID: https://orcid.org/0009-0005-2619-7221)
- Kristina A. Kostadinova (ORCID: https://orcid.org/0000-0003-2804-5924)
- Thomas Wharton (ORCID: https://orcid.org/0000-0002-9370-284X)
- David R. Spring (ORCID: https://orcid.org/0000-0001-7355-2824)
- Jason S. Carroll (ORCID: https://orcid.org/0000-0003-3643-0080)
- F. Javier Pérez-Areales (ORCID: https://orcid.org/0000-0001-9525-9346)
- Mahri Park (ORCID: https://orcid.org/0000-0003-3973-6026)
Institutions
- University of Cambridge (GB)
- Cancer Research UK (GB)
- Cancer Research UK Cambridge Center (GB)
Publication Details
- Journal
- Chemical Communications
- Published
- 2025-01-01
- DOI
- https://doi.org/10.1039/d5cc05824d
- Primary Topic
- HER2/EGFR in Cancer Research
- Type
- article
- Field-Weighted Citation Impact
- 0.00