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Molecules 2015, 20(9), 17511-17532;

G-Quadruplex Forming Oligonucleotides as Anti-HIV Agents

Department of Chemical Sciences, University of Napoli Federico II, via Cintia 21, Napoli I-80126, Italy
Author to whom correspondence should be addressed.
Academic Editor: Ramon Eritja
Received: 31 July 2015 / Revised: 10 September 2015 / Accepted: 16 September 2015 / Published: 22 September 2015
(This article belongs to the Special Issue Frontiers in Nucleic Acid Chemistry)
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Though a variety of different non-canonical nucleic acids conformations have been recognized, G-quadruplex structures are probably the structural motifs most commonly found within known oligonucleotide-based aptamers. This could be ascribed to several factors, as their large conformational diversity, marked responsiveness of their folding/unfolding processes to external stimuli, high structural compactness and chemo-enzymatic and thermodynamic stability. A number of G-quadruplex-forming oligonucleotides having relevant in vitro anti-HIV activity have been discovered in the last two decades through either SELEX or rational design approaches. Improved aptamers have been obtained by chemical modifications of natural oligonucleotides, as terminal conjugations with large hydrophobic groups, replacement of phosphodiester linkages with phosphorothioate bonds or other surrogates, insertion of base-modified monomers, etc. In turn, detailed structural studies have elucidated the peculiar architectures adopted by many G-quadruplex-based aptamers and provided insight into their mechanism of action. An overview of the state-of-the-art knowledge of the relevance of putative G-quadruplex forming sequences within the viral genome and of the most studied G-quadruplex-forming aptamers, selectively targeting HIV proteins, is here presented. View Full-Text
Keywords: G-quadruplex; modified oligonucleotides; anti-HIV agents; aptamers G-quadruplex; modified oligonucleotides; anti-HIV agents; aptamers

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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 (CC BY 4.0).

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Musumeci, D.; Riccardi, C.; Montesarchio, D. G-Quadruplex Forming Oligonucleotides as Anti-HIV Agents. Molecules 2015, 20, 17511-17532.

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