Molecular Engineering‐Based Aptamer–Drug Conjugates with Accurate Tunability of Drug Ratios for Drug Combination Targeted Cancer Therapy. Issue 34 (19th July 2019)

• Record Type: Journal Article
• Authors: Zhou, Fang; Wang, Peng; Peng, Yongbo; Zhang, Pengge; Huang, Qin; Sun, Weidi; He, Nongyue; Fu, Ting; Zhao, Zilong; Fang, Xiaohong; Tan, Weihong
• Is Part Of: Angewandte Chemie international edition. Volume 58:Issue 34(2019)
• Page Start: 11661
• Page End: 11665
• Publication Date: 2019-07-19
• Subjects: aptamers -- aptamer–drug conjugates -- drug combination cancer therapy -- drug delivery -- molecular engineering; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201903807
• Languages: English
• ISSNs: 1433-7851

Abstract

Abstract: 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. Abstract : Ratio(nal) delivery : Circular bivalent aptamer–drug conjugates (cb‐ApDCs) for drug combination cancer therapy have been developed. The cb‐ApDCs offer high stability, specific recognition, excellent cellular uptake, esterase‐triggered release, and tunable the drug ratios for an enhanced synergistic effect.