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Title: Cancer-targeted design of bioresponsive prodrug with enhanced cellular uptake to achieve precise cancer therapy
Authors: Liang, Yuanwei
Huang, Wei
Zeng, Delong
Huang, Xiaoting
Chan, Leung
Mei, Chaoming
Feng, Pengju
Tan, Choon-Hong
Chen, Tianfeng
Keywords: Science::Chemistry::Biochemistry
Adverse Effects
Issue Date: 2018
Source: Liang, Y., Huang, W., Zeng, D., Huang, X., Chan, L., Mei, C., . . . Chen, T. (2018). Cancer-targeted design of bioresponsive prodrug with enhanced cellular uptake to achieve precise cancer therapy. Drug Delivery, 25(1), 1350-1361. doi:10.1080/10717544.2018.1477862
Series/Report no.: Drug Delivery
Abstract: Chemical drug design based on the biochemical characteristics of cancer cells has become an important strategy for discovery of novel anticancer drugs to enhance the cancer targeting effects and biocompatibility, and decrease toxic side effects. Camptothecin (CPT) demonstrated strong anticancer activity in clinical trials but also notorious adverse effects. In this study, we presented a smart targeted delivery system (Biotin-ss-CPT) that consists of cancer-targeted moiety (biotin), a cleavable disulfide linker (S-S bond) and the active drug CPT. Biotin-ss-CPT was found to exhibit potent effects on the migration of cancer cells and induced apoptosis by induction of ROS-mediated mitochondrial dysfunction and perturbation of GSH/GPXs system, as well as activation of caspases. In vivo tumor suppression investigation including toxicity evaluation and pathology analysis, accompanied by MR images showed that Biotin-ss-CPT can be recognized specifically and selectively and taken up preferentially by cancers cells, followed by localization and accumulation effectively in tumor site, then released CPT by biological response to achieve high therapeutic effect and remarkably reduced the side effects that free CPT caused, such as liver damage, renal injury, and weight loss to realize precise cancer therapy. Taken together, our results suggest that biotinylation and bioresponsive functionalization of anticancer drugs could be a good way for the discovery of next-generation cancer therapeutics.
ISSN: 1071-7544
DOI: 10.1080/10717544.2018.1477862
Schools: School of Physical and Mathematical Sciences 
Rights: © 2018 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SPMS Journal Articles

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