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Computational repurposing of tamibarotene against triple mutant variant of SARS-CoV-2

The outbreak of the triple mutant strain of severe acute respiratory syndrome coronavirus-2 (SARS-COV-2) was more virulent and pathogenic than its original strain. The viral triple mutant strain of SARS-COV-2 is extremely adaptive and increases penetrability into the host. The triple mutant viral st...

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Autor principal: Mujwar, Somdutt
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8349365/
https://www.ncbi.nlm.nih.gov/pubmed/34388463
http://dx.doi.org/10.1016/j.compbiomed.2021.104748
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author Mujwar, Somdutt
author_facet Mujwar, Somdutt
author_sort Mujwar, Somdutt
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description The outbreak of the triple mutant strain of severe acute respiratory syndrome coronavirus-2 (SARS-COV-2) was more virulent and pathogenic than its original strain. The viral triple mutant strain of SARS-COV-2 is extremely adaptive and increases penetrability into the host. The triple mutant viral strain was first reported in Brazil and South Africa and then communicated to different countries responsible for the second wave of the coronavirus disease (COVID-19) global pandemic with a high mortality rate. The reported genomic mutations are responsible for the alterations in the viral functional and structural proteins, causing the ineffectiveness of the existing antiviral therapy targeting these proteins. Thus, in current research, molecular docking simulation-based virtual screening of a ligand library consisting of FDA-approved existing drugs followed by molecular dynamics simulation-based validation of leads was performed to develop a potent inhibitor molecule for the triple mutant viral strain SARS-CoV-2. Based on the safety profile, tamibarotene was selected as a safe and effective drug candidate for developing therapy against the triple mutant viral spike protein of SARS-CoV-2.
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spelling pubmed-83493652021-08-09 Computational repurposing of tamibarotene against triple mutant variant of SARS-CoV-2 Mujwar, Somdutt Comput Biol Med Article The outbreak of the triple mutant strain of severe acute respiratory syndrome coronavirus-2 (SARS-COV-2) was more virulent and pathogenic than its original strain. The viral triple mutant strain of SARS-COV-2 is extremely adaptive and increases penetrability into the host. The triple mutant viral strain was first reported in Brazil and South Africa and then communicated to different countries responsible for the second wave of the coronavirus disease (COVID-19) global pandemic with a high mortality rate. The reported genomic mutations are responsible for the alterations in the viral functional and structural proteins, causing the ineffectiveness of the existing antiviral therapy targeting these proteins. Thus, in current research, molecular docking simulation-based virtual screening of a ligand library consisting of FDA-approved existing drugs followed by molecular dynamics simulation-based validation of leads was performed to develop a potent inhibitor molecule for the triple mutant viral strain SARS-CoV-2. Based on the safety profile, tamibarotene was selected as a safe and effective drug candidate for developing therapy against the triple mutant viral spike protein of SARS-CoV-2. Elsevier Ltd. 2021-09 2021-08-08 /pmc/articles/PMC8349365/ /pubmed/34388463 http://dx.doi.org/10.1016/j.compbiomed.2021.104748 Text en © 2021 Elsevier Ltd. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Article
Mujwar, Somdutt
Computational repurposing of tamibarotene against triple mutant variant of SARS-CoV-2
title Computational repurposing of tamibarotene against triple mutant variant of SARS-CoV-2
title_full Computational repurposing of tamibarotene against triple mutant variant of SARS-CoV-2
title_fullStr Computational repurposing of tamibarotene against triple mutant variant of SARS-CoV-2
title_full_unstemmed Computational repurposing of tamibarotene against triple mutant variant of SARS-CoV-2
title_short Computational repurposing of tamibarotene against triple mutant variant of SARS-CoV-2
title_sort computational repurposing of tamibarotene against triple mutant variant of sars-cov-2
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8349365/
https://www.ncbi.nlm.nih.gov/pubmed/34388463
http://dx.doi.org/10.1016/j.compbiomed.2021.104748
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