Journal
CCS CHEMISTRY
Volume 1, Issue 2, Pages 226-236Publisher
CHINESE CHEMICAL SOC
DOI: 10.31635/ccschem.019.20180038
Keywords
antibody-drug conjugates; bioorthogonal prodrug; iEDDA reaction; enhanced tumor penetration; alleviated side effects
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Current antibody-drug conjugates (ADCs) suffer from low tissue penetration and significant side effects, largely due to the permanent linkage and/or premature release of cytotoxic payloads. Herein, we developed a prodrug-antibody conjugate (ProADC) strategy by conjugating a bioorthogonal-activatable prodrug with an antibody that allowed on-target release and on-demand activation of cytotoxic drugs at a tumor site. The bioorthogonal-caged prodrug exhibited an enhanced permeability into and on-demand activation within cancer cells, while the pH-sensitive ADC linker allowed on-target release of the anticancer agent. Together, the ProADCs showed enhanced tumor penetration and alleviated side effects for use as an on-target and on-demand chemotherapy agents.
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