期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 61, 期 26, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202202855
关键词
Anti-HER2 Therapy; Bio-orthogonal Reaction; Catalytic Metallodrug; Chemotherapy; Ruthenium Complex
资金
- National Natural Science Foundation of China [22022706, 22077142, 21837006, 91953117, 21877131]
- Natural Science Foundation of Guangdong Province, China [2019A1515011156]
- Fundamental Research Funds for the Central Universities
This study reports an anti-HER2 affibody-ruthenium catalyst hybrid that selectively catalyzes the activation of gemcitabine prodrug on tumor cells, resulting in suppression of tumor growth and reduced side effects.
Transition-metal catalysts exhibit great potential as therapeutic agents to inhibit tumor growth. However, the precise delivery and in situ catalysis are challenging in catalytic medicine. Herein, we report an anti-HER2 affibody-ruthenium catalyst hybrid, named Ru-HER2 for selective and effective killing of cancer cells. Ru-HER2 binds to the HER2 receptor on a tumor cell and in situ catalyzes the activation of gemcitabine prodrug, resulting in enhanced selectivity in suppression of tumor growth and reduction of side effects. Immunoblotting reveals that Ru-HER2 in combination with gemcitabine prodrug can not only induce DNA damage, but also effectively block the HER2 signaling pathway in cancer cells. Therefore, the HER2-targeted chemotherapy exhibits substantially high anticancer activity toward HER2-positive cancer cells in vitro and in vivo. In a word, we report the first affibody-ruthenium catalyst hybrid and reveal its potential for effective HER2-targeted cancer chemotherapy.
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