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Hotoda’s Sequence and Anti-HIV Activity: Where Are We Now?

The pharmacological relevance of ODNs forming G-quadruplexes as anti-HIV agents has been extensively reported in the literature over the last few years. Recent detailed studies have elucidated the peculiar arrangement adopted by many G-quadruplex-based aptamers and provided insight into their mechan...

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Autores principales: Romanucci, Valeria, Zarrelli, Armando, Di Fabio, Giovanni
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6479790/
https://www.ncbi.nlm.nih.gov/pubmed/30974914
http://dx.doi.org/10.3390/molecules24071417
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author Romanucci, Valeria
Zarrelli, Armando
Di Fabio, Giovanni
author_facet Romanucci, Valeria
Zarrelli, Armando
Di Fabio, Giovanni
author_sort Romanucci, Valeria
collection PubMed
description The pharmacological relevance of ODNs forming G-quadruplexes as anti-HIV agents has been extensively reported in the literature over the last few years. Recent detailed studies have elucidated the peculiar arrangement adopted by many G-quadruplex-based aptamers and provided insight into their mechanism of action. In this review, we have reported the history of a strong anti-HIV agent: the 6-mer d(TGGGAG) sequence, commonly called “Hotoda’s sequence”. In particular, all findings reported on this sequence and its modified sequences have been discussed considering the following research phases: (i) discovery of the first 5′-modified active d(TGGGAG) sequences; (ii) synthesis of a variety of end-modified d(TGGGAG) sequences; (iii) biophysical and NMR investigations of natural and modified Hotoda’s sequences; (iv); kinetic studies on the most active 5′-modified d(TGGGAG) sequences; and (v) extensive anti-HIV screening of G-quadruplexes formed by d(TGGGAG) sequences. This review aims to clarify all results obtained over the years on Hotoda’s sequence, revealing its potentiality as a strong anti-HIV agent (EC(50) = 14 nM).
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spelling pubmed-64797902019-04-30 Hotoda’s Sequence and Anti-HIV Activity: Where Are We Now? Romanucci, Valeria Zarrelli, Armando Di Fabio, Giovanni Molecules Review The pharmacological relevance of ODNs forming G-quadruplexes as anti-HIV agents has been extensively reported in the literature over the last few years. Recent detailed studies have elucidated the peculiar arrangement adopted by many G-quadruplex-based aptamers and provided insight into their mechanism of action. In this review, we have reported the history of a strong anti-HIV agent: the 6-mer d(TGGGAG) sequence, commonly called “Hotoda’s sequence”. In particular, all findings reported on this sequence and its modified sequences have been discussed considering the following research phases: (i) discovery of the first 5′-modified active d(TGGGAG) sequences; (ii) synthesis of a variety of end-modified d(TGGGAG) sequences; (iii) biophysical and NMR investigations of natural and modified Hotoda’s sequences; (iv); kinetic studies on the most active 5′-modified d(TGGGAG) sequences; and (v) extensive anti-HIV screening of G-quadruplexes formed by d(TGGGAG) sequences. This review aims to clarify all results obtained over the years on Hotoda’s sequence, revealing its potentiality as a strong anti-HIV agent (EC(50) = 14 nM). MDPI 2019-04-10 /pmc/articles/PMC6479790/ /pubmed/30974914 http://dx.doi.org/10.3390/molecules24071417 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Romanucci, Valeria
Zarrelli, Armando
Di Fabio, Giovanni
Hotoda’s Sequence and Anti-HIV Activity: Where Are We Now?
title Hotoda’s Sequence and Anti-HIV Activity: Where Are We Now?
title_full Hotoda’s Sequence and Anti-HIV Activity: Where Are We Now?
title_fullStr Hotoda’s Sequence and Anti-HIV Activity: Where Are We Now?
title_full_unstemmed Hotoda’s Sequence and Anti-HIV Activity: Where Are We Now?
title_short Hotoda’s Sequence and Anti-HIV Activity: Where Are We Now?
title_sort hotoda’s sequence and anti-hiv activity: where are we now?
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6479790/
https://www.ncbi.nlm.nih.gov/pubmed/30974914
http://dx.doi.org/10.3390/molecules24071417
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