Peroxide-cleavable linkers for antibody–drug conjugates†
Nicola
Ashman, 
a
Jonathan D.
Bargh,
a
Stephen J.
Walsh,
ab
Jason S.
Carroll
b
and
David R.
Spring
*a
a
Jonathan D.
Bargh,
a
Stephen J.
Walsh,
ab
Jason S.
Carroll
b
and
David R.
Spring
*a
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 in vitro.
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