期刊
CHEMICAL SCIENCE
卷 8, 期 3, 页码 2191-2198出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6sc03859j
关键词
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资金
- National Basic Research Program of China [2015CB856503]
- NSFC [31571011, 81301311, 51622305, 81220108015]
- PCSIRT [IRT13023]
- Science & Technology Project of Tianjin of China [15JCYBJC29800]
- University Grants Committee of Hong Kong [AoE/P-03/08]
- Research Grants Council of Hong Kong [16301614, 16305015, N_HKUST604/14]
- Innovation and Technology Commission [ITC-CNERC14SC01, RE: ITCPD/17-9]
- Singapore National Research Foundation [R-279-000-444-281]
- National University of Singapore [R279-000-482-133]
- Guangdong Innovative Research Team Program of China [201101C0105067115]
Photosensitizers are generally treated as key components for photodynamic therapy. In contrast, we herein report an aggregation-induced emission luminogen (AIEgen)-based photosensitizer (TPE-Py-FFGYSA) that can serve as a non-toxic adjuvant to amplify the antitumor efficacy of paclitaxel, a well-known anticancer drug, with a synergistic effect of 0 + 1 > 1. Besides the adjuvant function, TPE-Py-FFGYSA can selectively light up EphA2 protein clusters overexpressed in cancer cells in a fluorescence turn-on mode, by taking advantage of the specific YSA peptide (YSAYPDSVPMMS)-EphA2 protein interaction. The simple incorporation of FFG as a self-assembly-aided unit between AIEgen (TPE-Py) and YSA significantly enhances the fluorescent signal output of TPE-Py when imaging EphA2 clusters in live cancer cells. Cytotoxicity and western blot studies reveal that the reactive oxygen species (ROS) generated by TPEPy-FFGYSA upon exposure to light do not kill cancer cells, but instead provide an intracellular oxidative environment to help paclitaxel have much better efficacy. This study thus not only extends the application scope of photosensitizers, but also offers a unique theranostic system with the combination of diagnostic imaging and adjuvant antitumor therapy.
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