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Molecular Engineering‐Based Aptamer–Drug Conjugates with Accurate Tunability of Drug Ratios for Drug Combination Targeted Cancer Therapy
Author(s) -
Zhou Fang,
Wang Peng,
Peng Yongbo,
Zhang Pengge,
Huang Qin,
Sun Weidi,
He gyue,
Fu Ting,
Zhao Zilong,
Fang Xiaohong,
Tan Weihong
Publication year - 2019
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201903807
Subject(s) - drug , aptamer , drug delivery , conjugate , targeted drug delivery , drug resistance , pharmacology , chemistry , cancer therapy , cancer , combinatorial chemistry , medicine , nanotechnology , materials science , biology , microbiology and biotechnology , mathematics , mathematical analysis
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.