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Inhibitors of VPS34 and lipid metabolism suppress SARS-CoV-2 replication

Therapeutics targeting replication of SARS coronavirus 2 (SARS-CoV-2) are urgently needed. Coronaviruses rely on host membranes for entry, establishment of replication centers and egress. Compounds targeting cellular membrane biology and lipid biosynthetic pathways have previously shown promise as a...

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Autores principales: Silvas, Jesus A., Jureka, Alexander S., Nicolini, Anthony M., Chvatal, Stacie A., Basler, Christopher F.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Cold Spring Harbor Laboratory 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7386504/
https://www.ncbi.nlm.nih.gov/pubmed/32743584
http://dx.doi.org/10.1101/2020.07.18.210211
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author Silvas, Jesus A.
Jureka, Alexander S.
Nicolini, Anthony M.
Chvatal, Stacie A.
Basler, Christopher F.
author_facet Silvas, Jesus A.
Jureka, Alexander S.
Nicolini, Anthony M.
Chvatal, Stacie A.
Basler, Christopher F.
author_sort Silvas, Jesus A.
collection PubMed
description Therapeutics targeting replication of SARS coronavirus 2 (SARS-CoV-2) are urgently needed. Coronaviruses rely on host membranes for entry, establishment of replication centers and egress. Compounds targeting cellular membrane biology and lipid biosynthetic pathways have previously shown promise as antivirals and are actively being pursued as treatments for other conditions. Here, we tested small molecule inhibitors that target membrane dynamics or lipid metabolism. Included were inhibitors of the PI3 kinase VPS34, which functions in autophagy, endocytosis and other processes; Orlistat, an inhibitor of lipases and fatty acid synthetase, is approved by the FDA as a treatment for obesity; and Triacsin C which inhibits long chain fatty acyl-CoA synthetases. VPS34 inhibitors, Orlistat and Triacsin C inhibited virus growth in Vero E6 cells and in the human airway epithelial cell line Calu-3, acting at a post-entry step in the virus replication cycle. Of these the VPS34 inhibitors exhibit the most potent activity.
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spelling pubmed-73865042020-07-31 Inhibitors of VPS34 and lipid metabolism suppress SARS-CoV-2 replication Silvas, Jesus A. Jureka, Alexander S. Nicolini, Anthony M. Chvatal, Stacie A. Basler, Christopher F. bioRxiv Article Therapeutics targeting replication of SARS coronavirus 2 (SARS-CoV-2) are urgently needed. Coronaviruses rely on host membranes for entry, establishment of replication centers and egress. Compounds targeting cellular membrane biology and lipid biosynthetic pathways have previously shown promise as antivirals and are actively being pursued as treatments for other conditions. Here, we tested small molecule inhibitors that target membrane dynamics or lipid metabolism. Included were inhibitors of the PI3 kinase VPS34, which functions in autophagy, endocytosis and other processes; Orlistat, an inhibitor of lipases and fatty acid synthetase, is approved by the FDA as a treatment for obesity; and Triacsin C which inhibits long chain fatty acyl-CoA synthetases. VPS34 inhibitors, Orlistat and Triacsin C inhibited virus growth in Vero E6 cells and in the human airway epithelial cell line Calu-3, acting at a post-entry step in the virus replication cycle. Of these the VPS34 inhibitors exhibit the most potent activity. Cold Spring Harbor Laboratory 2020-07-20 /pmc/articles/PMC7386504/ /pubmed/32743584 http://dx.doi.org/10.1101/2020.07.18.210211 Text en http://creativecommons.org/licenses/by-nc-nd/4.0/It is made available under a CC-BY-NC-ND 4.0 International license (http://creativecommons.org/licenses/by-nc-nd/4.0/) .
spellingShingle Article
Silvas, Jesus A.
Jureka, Alexander S.
Nicolini, Anthony M.
Chvatal, Stacie A.
Basler, Christopher F.
Inhibitors of VPS34 and lipid metabolism suppress SARS-CoV-2 replication
title Inhibitors of VPS34 and lipid metabolism suppress SARS-CoV-2 replication
title_full Inhibitors of VPS34 and lipid metabolism suppress SARS-CoV-2 replication
title_fullStr Inhibitors of VPS34 and lipid metabolism suppress SARS-CoV-2 replication
title_full_unstemmed Inhibitors of VPS34 and lipid metabolism suppress SARS-CoV-2 replication
title_short Inhibitors of VPS34 and lipid metabolism suppress SARS-CoV-2 replication
title_sort inhibitors of vps34 and lipid metabolism suppress sars-cov-2 replication
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7386504/
https://www.ncbi.nlm.nih.gov/pubmed/32743584
http://dx.doi.org/10.1101/2020.07.18.210211
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