Towards a glutathione-cleavable azobenzene linker for antibody–drug conjugates
Mahri
Park, 
a
F. Javier
Pérez-Areales,
a
Kristina A.
Kostadinova,
a
Thomas
Wharton,
a
David R.
Spring
*a
a
F. Javier
Pérez-Areales,
a
Kristina A.
Kostadinova,
a
Thomas
Wharton,
a
David R.
Spring
*a
Abstract
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 in vitro cytotoxicity and selective activity towards HER2-positive cell lines.
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