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Development of Phosphorothioate DNA and DNA Thioaptamers

McGovern Medical School, Brown Foundation Institute of Molecular Medicine for the Prevention of Human Diseases, University of Texas Health Science Center, Houston, TX 77030, USA
Author to whom correspondence should be addressed.
Biomedicines 2017, 5(3), 41;
Received: 30 May 2017 / Revised: 3 July 2017 / Accepted: 11 July 2017 / Published: 13 July 2017
(This article belongs to the Special Issue Engineering Aptamers for Biomedical Applications)
Nucleic acid aptamers are short RNA- or DNA-based affinity reagents typically selected from combinatorial libraries to bind to a specific target such as a protein, a small molecule, whole cells or even animals. Aptamers have utility in the development of diagnostic, imaging and therapeutic applications due to their size, physico-chemical nature and ease of synthesis and modification to suit the application. A variety of oligonucleotide modifications have been used to enhance the stability of aptamers from nuclease degradation in vivo. The non-bridging oxygen atoms of the phosphodiester backbones of RNA and DNA aptamers can be substituted with one or two sulfur atoms, resulting in thioaptamers with phosphorothioate or phosphorodithioate linkages, respectively. Such thioaptamers are known to have increased binding affinity towards their target, as well as enhanced resistance to nuclease degradation. In this review, we discuss the development of phosphorothioate chemistry and thioaptamers, with a brief review of selection methods. View Full-Text
Keywords: DNA aptamer; thioaptamer; X-aptamer DNA aptamer; thioaptamer; X-aptamer
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MDPI and ACS Style

Volk, D.E.; Lokesh, G.L.R. Development of Phosphorothioate DNA and DNA Thioaptamers. Biomedicines 2017, 5, 41.

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