科研之友
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摘要
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.(#br)An affibody‐ruthenium catalyst hybrid (Ru‐HER2) binds to the HER2 receptor on cancer cells and catalyzes the in situ activation of gemcitabine prodrug, resulting in enhanced anticancer activity via the synergism between the HER2 signaling pathway blockade and gemcitabine‐induced DNA damage. Therefore, the catalytic chemotherapy selectively inhibits the growth of HER2‐positive cancer cells and significantly reduces the side effects to normal cells.
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