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Biomedicines. 2017 Aug 09;5(3). doi: 10.3390/biomedicines5030045.

Aptamer-siRNA Chimeras: Discovery, Progress, and Future Prospects.

Biomedicines

Sven Kruspe, Paloma H Giangrande

Affiliations

  1. Internal Medicine, University of Iowa, Iowa City, IA 52242, USA. [email protected].
  2. Internal Medicine, University of Iowa, Iowa City, IA 52242, USA. [email protected].
  3. Molecular & Cellular Biology Program, Holden Comprehensive Cancer Center, Radiation Oncology, Abboud Cardiovascular Research Center, and Environmental Health Sciences Research Center (EHSRC), University of Iowa, Iowa City, IA 52242, USA. [email protected].

PMID: 28792479 PMCID: PMC5618303 DOI: 10.3390/biomedicines5030045

Abstract

Synthetic nucleic acid ligands (aptamers) have emerged as effective delivery tools for many therapeutic oligonucleotide-based drugs, including small interfering RNAs (siRNAs). In this review, we summarize recent progress in the aptamer selection technology that has made possible the identification of cell-specific, cell-internalizing aptamers for the cell-targeted delivery of therapeutic oligonucleotides. In addition, we review the original, proof-of-concept aptamer-siRNA delivery studies and discuss recent advances in aptamer-siRNA conjugate designs for applications ranging from cancer therapy to the development of targeted antivirals. Challenges and prospects of aptamer-targeted siRNA drugs for clinical development are further highlighted.

Keywords: RNA interference; aptamers; targeted therapy

Conflict of interest statement

The authors declare no conflict of interest.

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