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

被引：146

作者：

He, Jiaxuan ^{[1
]}

Peng, Tianhuan ^{[1
]}

Peng, Yongbo ^{[1
]}

Ai, Lili ^{[1
]}

Deng, Zhengyu ^{[1
]}

Wang, Xue-Qiang ^{[1
]}

Tan, Weihong ^{[1
,2
,3
,4
,5
]}

机构：

[1] Hunan Univ, Changsha, Peoples R China

[2] Shanghai Jiao Tong Univ, Shanghai, Peoples R China

[3] Chinese Acad Sci, Hangzhou, Peoples R China

[4] Univ Chinese Acad Sci, Canc Hosp, Hangzhou, Peoples R China

[5] Fdn Appl Mol Evolut, Alachua, FL 32615 USA

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2020年 / 142卷 / 06期

关键词：

TARGETED DRUG-DELIVERY; NUCLEOLIN; CONJUGATE; FEATURES; AS1411;

D O I：

10.1021/jacs.9b10510

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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.

引用

收藏

页码：2699 / 2703

页数：5

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