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Structural Investigations and Binding Mechanisms of Oseltamivir Drug Resistance Conferred by the E119V Mutation in Influenza H7N9 Virus

The use of vaccinations and antiviral medications have gained popularity in the therapeutic management of avian influenza H7N9 virus lately. Antiviral medicines are more popular due to being readily available. The presence of the neuraminidase protein in the avian influenza H7N9 virus and its critic...

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Autores principales: Ugbaja, Samuel C., Mtambo, Sphamandla E., Mushebenge, Aganze G., Appiah-Kubi, Patrick, Abubakar, Bahijjahtu H., Ntuli, Mthobisi L., Kumalo, Hezekiel M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9317591/
https://www.ncbi.nlm.nih.gov/pubmed/35889251
http://dx.doi.org/10.3390/molecules27144376
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author Ugbaja, Samuel C.
Mtambo, Sphamandla E.
Mushebenge, Aganze G.
Appiah-Kubi, Patrick
Abubakar, Bahijjahtu H.
Ntuli, Mthobisi L.
Kumalo, Hezekiel M.
author_facet Ugbaja, Samuel C.
Mtambo, Sphamandla E.
Mushebenge, Aganze G.
Appiah-Kubi, Patrick
Abubakar, Bahijjahtu H.
Ntuli, Mthobisi L.
Kumalo, Hezekiel M.
author_sort Ugbaja, Samuel C.
collection PubMed
description The use of vaccinations and antiviral medications have gained popularity in the therapeutic management of avian influenza H7N9 virus lately. Antiviral medicines are more popular due to being readily available. The presence of the neuraminidase protein in the avian influenza H7N9 virus and its critical role in the cleavage of sialic acid have made it a target drug in the development of influenza virus drugs. Generally, the neuraminidase proteins have common conserved amino acid residues and any mutation that occurs around or within these conserved residues affects the susceptibility and replicability of the influenza H7N9 virus. Herein, we investigated the interatomic and intermolecular dynamic impacts of the experimentally reported E119V mutation on the oseltamivir resistance of the influenza H7N9 virus. We extensively employed molecular dynamic (MD) simulations and subsequent post-MD analyses to investigate the binding mechanisms of oseltamivir-neuraminidase wildtype and E119V mutant complexes. The results revealed that the oseltamivir-wildtype complex was more thermodynamically stable than the oseltamivir-E119V mutant complex. Oseltamivir exhibited a greater binding affinity for wildtype (−15.46 ± 0.23 kcal/mol) relative to the E119V mutant (−11.72 ± 0.21 kcal/mol). The decrease in binding affinity (−3.74 kcal/mol) was consistent with RMSD, RMSF, SASA, PCA, and hydrogen bonding profiles, confirming that the E119V mutation conferred lower conformational stability and weaker protein–ligand interactions. The findings of this oseltamivir-E119V mutation may further assist in the design of compounds to overcome E119V mutation in the treatment of influenza H7N9 virus patients.
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spelling pubmed-93175912022-07-27 Structural Investigations and Binding Mechanisms of Oseltamivir Drug Resistance Conferred by the E119V Mutation in Influenza H7N9 Virus Ugbaja, Samuel C. Mtambo, Sphamandla E. Mushebenge, Aganze G. Appiah-Kubi, Patrick Abubakar, Bahijjahtu H. Ntuli, Mthobisi L. Kumalo, Hezekiel M. Molecules Article The use of vaccinations and antiviral medications have gained popularity in the therapeutic management of avian influenza H7N9 virus lately. Antiviral medicines are more popular due to being readily available. The presence of the neuraminidase protein in the avian influenza H7N9 virus and its critical role in the cleavage of sialic acid have made it a target drug in the development of influenza virus drugs. Generally, the neuraminidase proteins have common conserved amino acid residues and any mutation that occurs around or within these conserved residues affects the susceptibility and replicability of the influenza H7N9 virus. Herein, we investigated the interatomic and intermolecular dynamic impacts of the experimentally reported E119V mutation on the oseltamivir resistance of the influenza H7N9 virus. We extensively employed molecular dynamic (MD) simulations and subsequent post-MD analyses to investigate the binding mechanisms of oseltamivir-neuraminidase wildtype and E119V mutant complexes. The results revealed that the oseltamivir-wildtype complex was more thermodynamically stable than the oseltamivir-E119V mutant complex. Oseltamivir exhibited a greater binding affinity for wildtype (−15.46 ± 0.23 kcal/mol) relative to the E119V mutant (−11.72 ± 0.21 kcal/mol). The decrease in binding affinity (−3.74 kcal/mol) was consistent with RMSD, RMSF, SASA, PCA, and hydrogen bonding profiles, confirming that the E119V mutation conferred lower conformational stability and weaker protein–ligand interactions. The findings of this oseltamivir-E119V mutation may further assist in the design of compounds to overcome E119V mutation in the treatment of influenza H7N9 virus patients. MDPI 2022-07-08 /pmc/articles/PMC9317591/ /pubmed/35889251 http://dx.doi.org/10.3390/molecules27144376 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Ugbaja, Samuel C.
Mtambo, Sphamandla E.
Mushebenge, Aganze G.
Appiah-Kubi, Patrick
Abubakar, Bahijjahtu H.
Ntuli, Mthobisi L.
Kumalo, Hezekiel M.
Structural Investigations and Binding Mechanisms of Oseltamivir Drug Resistance Conferred by the E119V Mutation in Influenza H7N9 Virus
title Structural Investigations and Binding Mechanisms of Oseltamivir Drug Resistance Conferred by the E119V Mutation in Influenza H7N9 Virus
title_full Structural Investigations and Binding Mechanisms of Oseltamivir Drug Resistance Conferred by the E119V Mutation in Influenza H7N9 Virus
title_fullStr Structural Investigations and Binding Mechanisms of Oseltamivir Drug Resistance Conferred by the E119V Mutation in Influenza H7N9 Virus
title_full_unstemmed Structural Investigations and Binding Mechanisms of Oseltamivir Drug Resistance Conferred by the E119V Mutation in Influenza H7N9 Virus
title_short Structural Investigations and Binding Mechanisms of Oseltamivir Drug Resistance Conferred by the E119V Mutation in Influenza H7N9 Virus
title_sort structural investigations and binding mechanisms of oseltamivir drug resistance conferred by the e119v mutation in influenza h7n9 virus
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9317591/
https://www.ncbi.nlm.nih.gov/pubmed/35889251
http://dx.doi.org/10.3390/molecules27144376
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