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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...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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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). |
format | Online Article Text |
id | pubmed-6479790 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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