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Issue 6, 2017
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Dual-targeted peptide-conjugated multifunctional fluorescent probe with AIEgen for efficient nucleus-specific imaging and long-term tracing of cancer cells

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Abstract

Precisely targeted transportation of a long-term tracing regent to a nucleus with low toxicity is one of the most challenging concerns in revealing cancer cell behaviors. Here, we report a dual-targeted peptide-conjugated multifunctional fluorescent probe (cNGR-CPP-NLS-RGD-PyTPE, TCNTP) with aggregation-induced emission (AIE) characteristic, for efficient nucleus-specific imaging and long-term and low-toxicity tracing of cancer cells. TCNTP mainly consists of two components: one is a functionalized combinatorial peptide (TCNT) containing two targeted peptides (cNGR and RGD), a cell-penetrating peptide (CPP) and a nuclear localization signal (NLS), which can specifically bind to a cell surface and effectively enter into the nucleus; the other one is an AIE-active tetraphenylethene derivative (PyTPE, a typical AIEgen) as fluorescence imaging reagent. In the presence of aminopeptidase N (CD13) and integrin αvβ3, TCNTP can specifically bind to both of them using cNGR and RGD, respectively, lighting up its yellow fluorescence. Because it contains CPP, TCNTP can be effectively integrated into the cytoplasm, and then be delivered into the nucleus with the help of NLS. TCNTP exhibited strong fluorescence in the nucleus of CD13 and integrin αvβ3 overexpression cells due to the specific targeting ability, efficient transport capacity and AIE characteristic in a more crowded space. Furthermore, TCNTP can be applied for long-term tracing in living cells, scarcely affecting normal cells with negligible toxicity in more than ten passages.

Graphical abstract: Dual-targeted peptide-conjugated multifunctional fluorescent probe with AIEgen for efficient nucleus-specific imaging and long-term tracing of cancer cells

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Publication details

The article was received on 26 Jan 2017, accepted on 19 Apr 2017 and first published on 19 Apr 2017


Article type: Edge Article
DOI: 10.1039/C7SC00402H
Citation: Chem. Sci., 2017,8, 4571-4578
  • Open access: Creative Commons BY license
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    Dual-targeted peptide-conjugated multifunctional fluorescent probe with AIEgen for efficient nucleus-specific imaging and long-term tracing of cancer cells

    Y. Cheng, C. Sun, X. Ou, B. Liu, X. Lou and F. Xia, Chem. Sci., 2017, 8, 4571
    DOI: 10.1039/C7SC00402H

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      [Original citation] - Published by The Royal Society of Chemistry.

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