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Peroxide-cleavable linkers for antibody-drug conjugates

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CHEMICAL COMMUNICATIONS
卷 59, 期 13, 页码 1841-1844

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ROYAL SOC CHEMISTRY
DOI: 10.1039/d2cc06677g

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Antibody-drug conjugates with peroxide-cleavable arylboronic acid linkers are developed to target cancer cells with high levels of reactive oxygen species (ROS). These linkers can rapidly release drugs in the presence of hydrogen peroxide while remaining stable in plasma. The peroxide-cleavable ADCs targeting HER2 and PD-L1 exhibit potent cytotoxicity in vitro.
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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