Oligonucleotide aptamers: New tools for targeted cancer therapy

Hongguang Sun, Xun Zhu, Patrick Y. Lu, Roberto R. Rosato, Wen Tan, Youli Zu

Research output: Contribution to journalReview articlepeer-review

442 Scopus citations


Aptamers are a class of small nucleic acid ligands that are composed of RNA or single-stranded DNA oligonucleotides and have high specificity and affinity for their targets. Similar to antibodies, aptamers interact with their targets by recognizing a specific three-dimensional structure and are thus termed "chemical antibodies." In contrast to protein antibodies, aptamers offer unique chemical and biological characteristics based on their oligonucleotide properties. Hence, they are more suitable for the development of novel clinical applications. Aptamer technology has been widely investigated in various biomedical fields for biomarker discovery, in vitro diagnosis, in vivo imaging, and targeted therapy. This review will discuss the potential applications of aptamer technology as a new tool for targeted cancer therapy with emphasis on the development of aptamers that are able to specifically target cell surface biomarkers. Additionally, we will describe several approaches for the use of aptamers in targeted therapeutics, including aptamer-drug conjugation, aptamer-nanoparticle conjugation, aptamer-mediated targeted gene therapy, aptamer-mediated immunotherapy, and aptamer-mediated biotherapy.

Original languageEnglish (US)
Article numbere182
JournalMolecular Therapy - Nucleic Acids
StatePublished - Aug 5 2014


  • cell surface biomarker
  • nanomedicine
  • oligonucleotide aptamer
  • targeted cancer therapy

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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