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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-mediated cancer therapy. Four approaches are presented: free aptamer as chemotherapeutic agents, aptamer-drug conjugates, aptamer-nanoparticle-drug delivery system and aptamer-guided cancer gene therapy. After specific binding of aptamers to their cell surface target, aptamer-conjugated therapeutic agents (including exogenous therapeutic nucleotides) or drug-encapsulated nanoparticles are internalised into cancer cells via receptor-mediated endocytosis. Subsequent escape from endosomes and/or lysosomes enables the released therapeutic agents to eradicate cancer cell.