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Issue 8, 2017
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A specific environment-sensitive near-infrared fluorescent turn-on probe for synergistic enhancement of anticancer activity of a chemo-drug

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Abstract

Chemotherapy is one of the main categories of clinical cancer treatment. One of the hindrances of a popularly used chemo-drug doxorubicin (DOX) is that some types of cancer cells are or become insensitive/resistant to DOX. In this work, we report a near-infrared (NIR) fluorescent turn-on probe DBT-2EEGYLFFVFER by conjugation of an environment-sensitive fluorophore DBT with human epidermal growth factor receptor 2 (HER2) specific binding peptides. Besides the NIR fluorescence turn-on signature, DBT-2EEGYLFFVFER also has activatable capability of reactive oxygen species (ROS) generation. DBT-2EEGYLFFVFER is weakly fluorescent in aqueous solution and hardly produces ROS under white light irradiation. However, both the NIR fluorescence and ROS production ability can be switched on when DBT-2EEGYLFFVFER binds to HER2 proteins overexpressed in cancer cells. Besides specific visualization of HER2-expressed cancer cells, DBT-2EEGYLFFVFER upon exposure to light is able to effectively increase the intracellular ROS level and offer an intracellular oxidative microenvironment, which does not cause the death of cancer cells, but greatly and synergistically boosts the cytotoxicity of DOX against HER2-expressed cancer cells with a supra-additive effect of “0 + 1 > 1”.

Graphical abstract: A specific environment-sensitive near-infrared fluorescent turn-on probe for synergistic enhancement of anticancer activity of a chemo-drug

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Publication details

The article was received on 28 Mar 2017, accepted on 15 May 2017 and first published on 19 May 2017


Article type: Paper
DOI: 10.1039/C7BM00270J
Citation: Biomater. Sci., 2017,5, 1622-1628
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    A specific environment-sensitive near-infrared fluorescent turn-on probe for synergistic enhancement of anticancer activity of a chemo-drug

    J. Li, Z. Zhu, S. Rong, H. Li, Y. Guo, Q. Xue and D. Ding, Biomater. Sci., 2017, 5, 1622
    DOI: 10.1039/C7BM00270J

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