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

Fangfei Li, Jun Lu, Jin Liu, Chao Liang, Maolin Wang, Luyao Wang, Defang Li, Houzong Yao, Qiulong Zhang, Jia Wen, Zong-Kang Zhang, Jie Li, Quanxia Lv, Xiaojuan He, Baosheng Guo, Daogang Guan, Yuanyuan Yu, Lei Dang, Xiaohao Wu, Yongshu Li, Guofen Chen, Feng Jiang, Shiguo Sun, Bao-Ting Zhang (), Aiping Lu () and Ge Zhang ()
Additional contact information
Fangfei Li: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University
Jun Lu: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University
Jin Liu: Institute for Advancing Translational Medicine in Bone and Joint Diseases (TMBJ), School of Chinese Medicine, Hong Kong Baptist University
Chao Liang: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University
Maolin Wang: Institute of Integrated Bioinfomedicine and Translational Science (IBTS), School of Chinese Medicine, Hong Kong Baptist University
Luyao Wang: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University
Defang Li: Institute for Advancing Translational Medicine in Bone and Joint Diseases (TMBJ), School of Chinese Medicine, Hong Kong Baptist University
Houzong Yao: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University
Qiulong Zhang: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University
Jia Wen: College of Science, Northwest Agriculture and Forestry University
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: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University
Xiaojuan He: Institute for Advancing Translational Medicine in Bone and Joint Diseases (TMBJ), School of Chinese Medicine, Hong Kong Baptist University
Baosheng Guo: Institute for Advancing Translational Medicine in Bone and Joint Diseases (TMBJ), School of Chinese Medicine, Hong Kong Baptist University
Daogang Guan: Institute of Integrated Bioinfomedicine and Translational Science (IBTS), School of Chinese Medicine, Hong Kong Baptist University
Yuanyuan Yu: Institute for Advancing Translational Medicine in Bone and Joint Diseases (TMBJ), School of Chinese Medicine, Hong Kong Baptist University
Lei Dang: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University
Xiaohao Wu: Institute for Advancing Translational Medicine in Bone and Joint Diseases (TMBJ), School of Chinese Medicine, Hong Kong Baptist University
Yongshu Li: Institute for Advancing Translational Medicine in Bone and Joint Diseases (TMBJ), School of Chinese Medicine, Hong Kong Baptist University
Guofen Chen: Nanfang Hospital
Feng Jiang: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University
Shiguo Sun: College of Science, Northwest Agriculture and Forestry University
Bao-Ting Zhang: School of Chinese Medicine, Faculty of Medicine, The Chinese University of Hong Kong
Aiping Lu: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University
Ge Zhang: Institute of Precision Medicine and Innovative Drug Discovery (PMID), School of Chinese Medicine, Hong Kong Baptist University

Nature Communications, 2017, vol. 8, issue 1, 1-14

Abstract: 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.

Date: 2017
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DOI: 10.1038/s41467-017-01565-6

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