BI-2 destabilizes HIV-1 cores during infection and Prevents Binding of CPSF6 to the HIV-1 Capsid

BACKGROUND: The recently discovered small-molecule BI-2 potently blocks HIV-1 infection. BI-2 binds to the N-terminal domain of HIV-1 capsid. BI-2 utilizes the same capsid pocket used by the small molecule PF74. Although both drugs bind to the same pocket, it has been proposed that BI-2 uses a diffe...

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Autores principales: Fricke, Thomas, Buffone, Cindy, Opp, Silvana, Valle-Casuso, Jose, Diaz-Griffero, Felipe
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2014
Materias:
Short Report
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4271331/
https://www.ncbi.nlm.nih.gov/pubmed/25496772
http://dx.doi.org/10.1186/s12977-014-0120-x
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author Fricke, Thomas
Buffone, Cindy
Opp, Silvana
Valle-Casuso, Jose
Diaz-Griffero, Felipe
author_facet Fricke, Thomas
Buffone, Cindy
Opp, Silvana
Valle-Casuso, Jose
Diaz-Griffero, Felipe
author_sort Fricke, Thomas
collection PubMed
description BACKGROUND: The recently discovered small-molecule BI-2 potently blocks HIV-1 infection. BI-2 binds to the N-terminal domain of HIV-1 capsid. BI-2 utilizes the same capsid pocket used by the small molecule PF74. Although both drugs bind to the same pocket, it has been proposed that BI-2 uses a different mechanism to block HIV-1 infection when compared to PF74. FINDINGS: This work demonstrates that BI-2 destabilizes the HIV-1 core during infection, and prevents the binding of the cellular factor CPSF6 to the HIV-1 core. CONCLUSIONS: Overall this short-form paper suggests that BI-2 is using a similar mechanism to the one used by PF74 to block HIV-1 infection.
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spelling pubmed-42713312014-12-20 BI-2 destabilizes HIV-1 cores during infection and Prevents Binding of CPSF6 to the HIV-1 Capsid Fricke, Thomas Buffone, Cindy Opp, Silvana Valle-Casuso, Jose Diaz-Griffero, Felipe Retrovirology Short Report BACKGROUND: The recently discovered small-molecule BI-2 potently blocks HIV-1 infection. BI-2 binds to the N-terminal domain of HIV-1 capsid. BI-2 utilizes the same capsid pocket used by the small molecule PF74. Although both drugs bind to the same pocket, it has been proposed that BI-2 uses a different mechanism to block HIV-1 infection when compared to PF74. FINDINGS: This work demonstrates that BI-2 destabilizes the HIV-1 core during infection, and prevents the binding of the cellular factor CPSF6 to the HIV-1 core. CONCLUSIONS: Overall this short-form paper suggests that BI-2 is using a similar mechanism to the one used by PF74 to block HIV-1 infection. BioMed Central 2014-12-11 /pmc/articles/PMC4271331/ /pubmed/25496772 http://dx.doi.org/10.1186/s12977-014-0120-x Text en © Fricke et al.; licensee BioMed Central Ltd. 2014 This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Short Report
Fricke, Thomas
Buffone, Cindy
Opp, Silvana
Valle-Casuso, Jose
Diaz-Griffero, Felipe
BI-2 destabilizes HIV-1 cores during infection and Prevents Binding of CPSF6 to the HIV-1 Capsid
title BI-2 destabilizes HIV-1 cores during infection and Prevents Binding of CPSF6 to the HIV-1 Capsid
title_full BI-2 destabilizes HIV-1 cores during infection and Prevents Binding of CPSF6 to the HIV-1 Capsid
title_fullStr BI-2 destabilizes HIV-1 cores during infection and Prevents Binding of CPSF6 to the HIV-1 Capsid
title_full_unstemmed BI-2 destabilizes HIV-1 cores during infection and Prevents Binding of CPSF6 to the HIV-1 Capsid
title_short BI-2 destabilizes HIV-1 cores during infection and Prevents Binding of CPSF6 to the HIV-1 Capsid
title_sort bi-2 destabilizes hiv-1 cores during infection and prevents binding of cpsf6 to the hiv-1 capsid
topic Short Report
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4271331/
https://www.ncbi.nlm.nih.gov/pubmed/25496772
http://dx.doi.org/10.1186/s12977-014-0120-x
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