Molecularly Engineering Triptolide with Aptamers for High Specificity and Cytotoxicity for Triple-Negative Breast Cancer

Triple-negative breast cancer (TNBC) lacks three important receptors, ER, PR, and HER2. It is more aggressive and more likely to relapse after treatment, thus has been identified as one of the most malignant breast cancer types. The development of efficient targeted TNBC therapy is an important rese...

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Bibliographic Details
Published in:Journal of the American Chemical Society 2020-02, Vol.142 (6), p.2699-2703
Main Authors: He, Jiaxuan, Peng, Tianhuan, Peng, Yongbo, Ai, Lili, Deng, Zhengyu, Wang, Xue-Qiang, Tan, Weihong
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antineoplastic Agents - therapeutic use
Apoptosis - drug effects
Aptamers, Nucleotide - chemistry
Cell Line, Tumor
Cell Proliferation - drug effects
Diterpenes - chemistry
Diterpenes - pharmacology
Diterpenes - therapeutic use
Epoxy Compounds - chemistry
Epoxy Compounds - pharmacology
Epoxy Compounds - therapeutic use
Female
Humans
Mice
Phenanthrenes - chemistry
Phenanthrenes - pharmacology
Phenanthrenes - therapeutic use
Triple Negative Breast Neoplasms - drug therapy
Triple Negative Breast Neoplasms - pathology
Xenograft Model Antitumor Assays
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Summary:Triple-negative breast cancer (TNBC) lacks three important receptors, ER, PR, and HER2. It is more aggressive and more likely to relapse after treatment, thus has been identified as one of the most malignant breast cancer types. The development of efficient targeted TNBC therapy is an important research topic in TNBC treatment. We report the development of a new aptamer–drug conjugate (ApDC), AS1411–triptolide conjugate (ATC), as targeted therapy for the treatment of TNBC with high efficacy. The conjugate possesses excellent specificity and high cytotoxicity against the MDA-MB-231 cell line. The advantages of our newly invented ATC are further highlighted by its excellent in vivo anti-TNBC efficacy and negligible side effects toward healthy organs.
ISSN:0002-7863
1520-5126
DOI:10.1021/jacs.9b10510