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Pharmaceuticals 2011, 4(11), 1434-1449; doi:10.3390/ph4111434

Coupling Aptamers to Short Interfering RNAs as Therapeutics

1,* , 1, 1,2, 1,2 and 1
1 Istituto per l’Endocrinologia e l’Oncologia Sperimentale del CNR “G. Salvatore”, Via S. Pansini 5, 80131 Naples, Italy 2 Dipartimento di Biologia e Patologia Cellulare e Molecolare, Università di Napoli “Federico II”, Via S. Pansini 5, 80131 Naples, Italy
* Author to whom correspondence should be addressed.
Received: 22 September 2011 / Revised: 13 October 2011 / Accepted: 24 October 2011 / Published: 27 October 2011
(This article belongs to the Special Issue Aptamer-Based Therapeutics)
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RNA-based approaches are among the most promising strategies aimed at developing safer and more effective therapeutics. RNA therapeutics include small non-coding miRNAs, small interfering RNA, RNA aptamers and more recently, small activating RNAs. However, major barriers exist to the use of RNAs as therapeutics such as resistance to nucleases present in biological fluids, poor chemical stability, need of specific cell targeted delivery and easy entry into the cell. Such issues have been addressed by several recent reports that show the possibility of introducing chemical modifications in small RNAs to stabilize the molecular conformation and increase by several fold their integrity, while still preserving the functional activity. Further, several aptamers have been developed as excellent candidates for the specific recognition of cell surface targets. In the last few years, by taking advantage of recent advances in the small RNA field, molecular bioconjugates have been designed that permit specific targeting and may act as cargoes for cell internalization of small RNAs acting on gene expression that will be discussed in this review.
Keywords: aptamer; intracellular delivery; microRNA; small interfering RNA aptamer; intracellular delivery; microRNA; small interfering RNA
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Cerchia, L.; Esposito, C.L.; Camorani, S.; Catuogno, S.; Franciscis, V. Coupling Aptamers to Short Interfering RNAs as Therapeutics. Pharmaceuticals 2011, 4, 1434-1449.

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