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Applications of Cancer Cell-Specific Aptamers in Targeted Delivery of Anticancer Therapeutic Agents

Department of Bioscience and Biotechnology, Konkuk University, Seoul 05029, Korea
Department of Biomedical Laboratory Science, Konyang University, Daejeon 35365, Korea
Department of Emergency Medicine Kyung Hee University Hospital at Gangdong, Seoul 05278, Korea
Author to whom correspondence should be addressed.
These two authors contributed equally.
Molecules 2018, 23(4), 830;
Received: 7 March 2018 / Revised: 30 March 2018 / Accepted: 2 April 2018 / Published: 4 April 2018
(This article belongs to the Special Issue Nucleic Acid Aptamers)
PDF [7808 KB, uploaded 3 May 2018]


Aptamers are single-stranded oligonucleotides that specifically bind and interact with their corresponding targets, including proteins and cells, through unique three-dimensional structures. Numerous aptamers have been developed to target cancer biomarkers with high specificity and affinity, and some are employed as versatile guiding ligands for cancer-specific drug delivery and anti-cancer therapeutics. In this review, we list the aptamers that target tumor surface biomarkers and summarize the representative applications of aptamers as agonists and antagonists that activate anti-cancer and inactivate pro-cancer biomarkers, respectively. In addition, we describe applications of aptamer-drug or aptamer-oligonucleotide conjugates that can deliver therapeutic agents, including small interfering RNAs, micro RNAs, short hairpin RNAs, and chemotherapeutic molecules, to cancer cells. Moreover, we provide examples of aptamer- conjugated nano-vehicles, in which cancer-targeting oligonucleotide aptamers are conjugated with nano-vehicles such as liposomes, micelles, polymeric nanoparticles, and quantum dots. Conjugation of aptamers with anti-cancer drugs and nano-vehicles will facilitate innovative applications of aptamer-based cancer therapeutics. View Full-Text
Keywords: aptamer; targeted delivery; targeted cancer therapy; aptamer conjugates aptamer; targeted delivery; targeted cancer therapy; aptamer conjugates

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Kim, M.; Kim, D.-M.; Kim, K.-S.; Jung, W.; Kim, D.-E. Applications of Cancer Cell-Specific Aptamers in Targeted Delivery of Anticancer Therapeutic Agents. Molecules 2018, 23, 830.

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