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From Acid Activation Mechanisms of Proton Conduction to Design of Inhibitors of the M2 Proton Channel of Influenza A Virus

With an estimated 1 billion people affected across the globe, influenza is one of the most serious health concerns worldwide. Therapeutic treatments have encompassed a number of key functional viral proteins, mainly focused on the M2 proton channel and neuraminidase. This review highlights the effor...

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Autores principales: Aledavood, Elnaz, Selmi, Beatrice, Estarellas, Carolina, Masetti, Matteo, Luque, F. Javier
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8795881/
https://www.ncbi.nlm.nih.gov/pubmed/35096969
http://dx.doi.org/10.3389/fmolb.2021.796229
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author Aledavood, Elnaz
Selmi, Beatrice
Estarellas, Carolina
Masetti, Matteo
Luque, F. Javier
author_facet Aledavood, Elnaz
Selmi, Beatrice
Estarellas, Carolina
Masetti, Matteo
Luque, F. Javier
author_sort Aledavood, Elnaz
collection PubMed
description With an estimated 1 billion people affected across the globe, influenza is one of the most serious health concerns worldwide. Therapeutic treatments have encompassed a number of key functional viral proteins, mainly focused on the M2 proton channel and neuraminidase. This review highlights the efforts spent in targeting the M2 proton channel, which mediates the proton transport toward the interior of the viral particle as a preliminary step leading to the release of the fusion peptide in hemagglutinin and the fusion of the viral and endosomal membranes. Besides the structural and mechanistic aspects of the M2 proton channel, attention is paid to the challenges posed by the development of efficient small molecule inhibitors and the evolution toward novel ligands and scaffolds motivated by the emergence of resistant strains.
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spelling pubmed-87958812022-01-29 From Acid Activation Mechanisms of Proton Conduction to Design of Inhibitors of the M2 Proton Channel of Influenza A Virus Aledavood, Elnaz Selmi, Beatrice Estarellas, Carolina Masetti, Matteo Luque, F. Javier Front Mol Biosci Molecular Biosciences With an estimated 1 billion people affected across the globe, influenza is one of the most serious health concerns worldwide. Therapeutic treatments have encompassed a number of key functional viral proteins, mainly focused on the M2 proton channel and neuraminidase. This review highlights the efforts spent in targeting the M2 proton channel, which mediates the proton transport toward the interior of the viral particle as a preliminary step leading to the release of the fusion peptide in hemagglutinin and the fusion of the viral and endosomal membranes. Besides the structural and mechanistic aspects of the M2 proton channel, attention is paid to the challenges posed by the development of efficient small molecule inhibitors and the evolution toward novel ligands and scaffolds motivated by the emergence of resistant strains. Frontiers Media S.A. 2022-01-14 /pmc/articles/PMC8795881/ /pubmed/35096969 http://dx.doi.org/10.3389/fmolb.2021.796229 Text en Copyright © 2022 Aledavood, Selmi, Estarellas, Masetti and Luque. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Molecular Biosciences
Aledavood, Elnaz
Selmi, Beatrice
Estarellas, Carolina
Masetti, Matteo
Luque, F. Javier
From Acid Activation Mechanisms of Proton Conduction to Design of Inhibitors of the M2 Proton Channel of Influenza A Virus
title From Acid Activation Mechanisms of Proton Conduction to Design of Inhibitors of the M2 Proton Channel of Influenza A Virus
title_full From Acid Activation Mechanisms of Proton Conduction to Design of Inhibitors of the M2 Proton Channel of Influenza A Virus
title_fullStr From Acid Activation Mechanisms of Proton Conduction to Design of Inhibitors of the M2 Proton Channel of Influenza A Virus
title_full_unstemmed From Acid Activation Mechanisms of Proton Conduction to Design of Inhibitors of the M2 Proton Channel of Influenza A Virus
title_short From Acid Activation Mechanisms of Proton Conduction to Design of Inhibitors of the M2 Proton Channel of Influenza A Virus
title_sort from acid activation mechanisms of proton conduction to design of inhibitors of the m2 proton channel of influenza a virus
topic Molecular Biosciences
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8795881/
https://www.ncbi.nlm.nih.gov/pubmed/35096969
http://dx.doi.org/10.3389/fmolb.2021.796229
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