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. 2015 Jan 1;5(1):23–42. doi: 10.7150/thno.10202

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© Ivyspring International Publisher. This is an open-access article distributed under the terms of the Creative Commons License (http://creativecommons.org/licenses/by-nc-nd/3.0/). Reproduction is permitted for personal, noncommercial use, provided that the article is in whole, unmodified, and properly cited.

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Schematic illustration of aptamer-guided cancer nucleic acid therapy. Exogenous therapeutic small RNAs (siRNA, miRNA and anti-miRNA) can be directly conjugated with aptamers or encapsulated within nanoparticles functionalized with an aptamer. As targeted-delivery modalities, aptamers bind to cell surface targets on cancer cells, followed by internalisation via receptor-mediated endocytosis. Through unknown mechanisms, small RNAs escape endosomes and engage cytoplasmic RNAi/miRNA protein machinery. The mature siRNA/shRNA/miRNA interact with their cytoplasmic or nucleic target sequences, leading to mRNA degradation, translation promotion or repression or modulation of gene expression.