Document Type

Journal Article

Authors

Fangfei Li, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Jun Lu, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Jin Liu, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Chao Liang, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Maolin Wang, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Luyao Wang, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Defang Li, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Houzong Yao, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Qiulong Zhang, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Jia Wen, College of Science, Northwest Agriculture and Forestry University, Yangling, China
Zong-Kang Zhang, School of Chinese Medicine, Faculty of Medicine, The Chinese University of Hong Kong
Jie Li, School of Chinese Medicine, Faculty of Medicine, The Chinese University of Hong Kong
Quanxia Lv, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Xiaojuan He, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Baosheng Guo, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong
Daogang Guan, School of Chinese Medicine, Hong Kong Baptist University
Yuanyuan Yu, School of Chinese Medicine, Hong Kong Baptist University
Lei Dang, School of Chinese Medicine, Hong Kong Baptist University
Xiaohao Wu, School of Chinese Medicine, Hong Kong Baptist University
Yongshu Li, School of Chinese Medicine, Hong Kong Baptist University
Guofen Chen, Department of Orthopaedics and Traumatology, Nanfang Hospital, Guangzhou, China
Feng Jiang, School of Chinese Medicine, Hong Kong Baptist University
Shiguo Sun, 4 College of Science, Northwest Agriculture and Forestry University, Yangling, China
Bao-Ting Zhang, School of Chinese Medicine, Faculty of Medicine, The Chinese University of Hong Kong
Aiping Lu, School of Chinese Medicine, Hong Kong Baptist University
Ge Zhang, School of Chinese Medicine, Hong Kong Baptist University

Department/Unit

School of Chinese Medicine

Title

A water-soluble nucleolin aptamer-paclitaxel conjugate for tumor-specific targeting in ovarian cancer

Language

English

Abstract

Paclitaxel (PTX) is among the most commonly used first-line drugs for cancer chemotherapy. However, its poor water solubility and indiscriminate distribution in normal tissues remain clinical challenges. Here we design and synthesize a highly water-soluble nucleolin aptamer-paclitaxel conjugate (NucA-PTX) that selectively delivers PTX to the tumor site. By connecting a tumor-targeting nucleolin aptamer (NucA) to the active hydroxyl group at 2′ position of PTX via a cathepsin B sensitive dipeptide bond, NucA-PTX remains stable and inactive in the circulation. NucA facilitates the uptake of the conjugated PTX specifically in tumor cells. Once inside cells, the dipeptide bond linker of NucA-PTX is cleaved by cathepsin B and then the conjugated PTX is released for action. The NucA modification assists the selective accumulation of the conjugated PTX in ovarian tumor tissue rather than normal tissues, and subsequently resulting in notably improved antitumor activity and reduced toxicity.

Publication Date

11-2017

Source Publication Title

Nature Communications

Volume

8

Publisher

Nature Research

Creative Commons License

Creative Commons Attribution 4.0 License
This work is licensed under a Creative Commons Attribution 4.0 License.

DOI

10.1038/s41467-017-01565-6

Link to Publisher's Edition

http://dx.doi.org/10.1038/s41467-017-01565-6

ISSN (electronic)

20411723

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