Bioorthogonal Prodrug–Antibody Conjugates for On-Target and On-Demand Chemotherapy | Zendy

Feng Lin | Zendy; Long Chen | Zendy; Heng Zhang | Zendy; William Shu Ching Ngai | Zendy; Xiangmei Zeng | Zendy; Jian Lin | Zendy; Peng R. Chen | Zendy

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Bioorthogonal Prodrug–Antibody Conjugates for On-Target and On-Demand Chemotherapy

Author(s) -

Feng Lin,

Long Chen,

Heng Zhang,

William Shu Ching Ngai,

Xiangmei Zeng,

Jian Lin,

Peng R. Chen

Publication year - 2019

Publication title -

ccs chemistry

Language(s) - English

Resource type - Journals

ISSN - 2096-5745

DOI - 10.31635/ccschem.019.20180038

Subject(s) - prodrug , bioorthogonal chemistry , conjugate , chemistry , linker , penetration (warfare) , cytotoxic t cell , cancer cell , pharmacology , combinatorial chemistry , biochemistry , cancer , medicine , click chemistry , in vitro , mathematical analysis , mathematics , operations research , computer science , engineering , operating system

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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