Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 58, Issue 34, Pages 11661-11665Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201903807
Keywords
aptamers; aptamer-drug conjugates; drug combination cancer therapy; drug delivery; molecular engineering
Categories
Funding
- NSFC [61527806, 21405041]
- State Key Laboratory of Chemo/Biosensing and Chemometrics
- Fundamental Research Funds for the Central Universities
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Polytherapy (or drug combination cancer therapy (DCCT)), targeting multiple mechanisms associated with tumor proliferation, can efficiently maximize therapeutic efficacy, decrease drug dosage, and reduce drug resistance. However, most DCCT strategies cannot coordinate the specific delivery of a drug combination in an accurately tuned ratio into cancer cells. To address these limitations, the present work reports the engineering of circular bivalent aptamer-drug conjugates (cb-ApDCs). The cb-ApDCs exhibit high stability, specific recognition, excellent cellular uptake, and esterase-triggered release. Furthermore, the drug ratios in cb-ApDCs can be tuned for an enhanced synergistic effect without the need for complex chemistry. Therefore, cb-ApDCs provide a promising platform for the development of DCCT strategies for different drug combinations and ratios.
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