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Pharmaceuticals 2010, 3(6), 1761-1778; doi:10.3390/ph3061761
Review

Aptamers for Targeted Drug Delivery

 and *
Received: 5 March 2010; in revised form: 19 May 2010 / Accepted: 26 May 2010 / Published: 27 May 2010
(This article belongs to the Special Issue Targeted Therapy)
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Abstract: Aptamers are a class of therapeutic oligonucleotides that form specific three-dimensional structures that are dictated by their sequences. They are typically generated by an iterative screening process of complex nucleic acid libraries employing a process termed Systemic Evolution of Ligands by Exponential Enrichment (SELEX). SELEX has traditionally been performed using purified proteins, and cell surface receptors may be challenging to purify in their properly folded and modified conformations. Therefore, relatively few aptamers have been generated that bind cell surface receptors. However, improvements in recombinant fusion protein technology have increased the availability of receptor extracellular domains as purified protein targets, and the development of cell-based selection techniques has allowed selection against surface proteins in their native configuration on the cell surface. With cell-based selection, a specific protein target is not always chosen, but selection is performed against a target cell type with the goal of letting the aptamer choose the target. Several studies have demonstrated that aptamers that bind cell surface receptors may have functions other than just blocking receptor-ligand interactions. All cell surface proteins cycle intracellularly to some extent, and many surface receptors are actively internalized in response to ligand binding. Therefore, aptamers that bind cell surface receptors have been exploited for the delivery of a variety of cargoes into cells. This review focuses on recent progress and current challenges in the field of aptamer-mediated delivery.
Keywords: Systemic Evolution of Ligands by Exponential Enrichment (SELEX); aptamers; targeted drug delivery Systemic Evolution of Ligands by Exponential Enrichment (SELEX); aptamers; targeted drug delivery
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Ray, P.; White, R.R. Aptamers for Targeted Drug Delivery. Pharmaceuticals 2010, 3, 1761-1778.

AMA Style

Ray P, White RR. Aptamers for Targeted Drug Delivery. Pharmaceuticals. 2010; 3(6):1761-1778.

Chicago/Turabian Style

Ray, Partha; White, Rebekah R. 2010. "Aptamers for Targeted Drug Delivery." Pharmaceuticals 3, no. 6: 1761-1778.


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