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BRD2 inhibition blocks SARS-CoV-2 infection by reducing transcription of the host cell receptor ACE2
SARS-CoV-2 infection of human cells is initiated by the binding of the viral Spike protein to its cell-surface receptor ACE2. We conducted a targeted CRISPRi screen to uncover druggable pathways controlling Spike protein binding to human cells. Here we show that the protein BRD2 is required for ACE2...
Autores principales: | , , , , , , , , , , , , , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8820466/ https://www.ncbi.nlm.nih.gov/pubmed/35027731 http://dx.doi.org/10.1038/s41556-021-00821-8 |
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author | Samelson, Avi J. Tran, Quang Dinh Robinot, Rémy Carrau, Lucia Rezelj, Veronica V. Kain, Alice Mac Chen, Merissa Ramadoss, Gokul N. Guo, Xiaoyan Lim, Shion A. Lui, Irene Nuñez, James K. Rockwood, Sarah J. Wang, Jianhui Liu, Na Carlson-Stevermer, Jared Oki, Jennifer Maures, Travis Holden, Kevin Weissman, Jonathan S. Wells, James A. Conklin, Bruce R. TenOever, Benjamin R. Chakrabarti, Lisa A. Vignuzzi, Marco Tian, Ruilin Kampmann, Martin |
author_facet | Samelson, Avi J. Tran, Quang Dinh Robinot, Rémy Carrau, Lucia Rezelj, Veronica V. Kain, Alice Mac Chen, Merissa Ramadoss, Gokul N. Guo, Xiaoyan Lim, Shion A. Lui, Irene Nuñez, James K. Rockwood, Sarah J. Wang, Jianhui Liu, Na Carlson-Stevermer, Jared Oki, Jennifer Maures, Travis Holden, Kevin Weissman, Jonathan S. Wells, James A. Conklin, Bruce R. TenOever, Benjamin R. Chakrabarti, Lisa A. Vignuzzi, Marco Tian, Ruilin Kampmann, Martin |
author_sort | Samelson, Avi J. |
collection | PubMed |
description | SARS-CoV-2 infection of human cells is initiated by the binding of the viral Spike protein to its cell-surface receptor ACE2. We conducted a targeted CRISPRi screen to uncover druggable pathways controlling Spike protein binding to human cells. Here we show that the protein BRD2 is required for ACE2 transcription in human lung epithelial cells and cardiomyocytes, and BRD2 inhibitors currently evaluated in clinical trials potently block endogenous ACE2 expression and SARS-CoV-2 infection of human cells, including those of human nasal epithelia. Moreover, pharmacological BRD2 inhibition with the drug ABBV-744 inhibited SARS-CoV-2 replication in Syrian hamsters. We also found that BRD2 controls transcription of several other genes induced upon SARS-CoV-2 infection, including the interferon response, which in turn regulates the antiviral response. Together, our results pinpoint BRD2 as a potent and essential regulator of the host response to SARS-CoV-2 infection and highlight the potential of BRD2 as a therapeutic target for COVID-19. |
format | Online Article Text |
id | pubmed-8820466 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
record_format | MEDLINE/PubMed |
spelling | pubmed-88204662022-07-13 BRD2 inhibition blocks SARS-CoV-2 infection by reducing transcription of the host cell receptor ACE2 Samelson, Avi J. Tran, Quang Dinh Robinot, Rémy Carrau, Lucia Rezelj, Veronica V. Kain, Alice Mac Chen, Merissa Ramadoss, Gokul N. Guo, Xiaoyan Lim, Shion A. Lui, Irene Nuñez, James K. Rockwood, Sarah J. Wang, Jianhui Liu, Na Carlson-Stevermer, Jared Oki, Jennifer Maures, Travis Holden, Kevin Weissman, Jonathan S. Wells, James A. Conklin, Bruce R. TenOever, Benjamin R. Chakrabarti, Lisa A. Vignuzzi, Marco Tian, Ruilin Kampmann, Martin Nat Cell Biol Article SARS-CoV-2 infection of human cells is initiated by the binding of the viral Spike protein to its cell-surface receptor ACE2. We conducted a targeted CRISPRi screen to uncover druggable pathways controlling Spike protein binding to human cells. Here we show that the protein BRD2 is required for ACE2 transcription in human lung epithelial cells and cardiomyocytes, and BRD2 inhibitors currently evaluated in clinical trials potently block endogenous ACE2 expression and SARS-CoV-2 infection of human cells, including those of human nasal epithelia. Moreover, pharmacological BRD2 inhibition with the drug ABBV-744 inhibited SARS-CoV-2 replication in Syrian hamsters. We also found that BRD2 controls transcription of several other genes induced upon SARS-CoV-2 infection, including the interferon response, which in turn regulates the antiviral response. Together, our results pinpoint BRD2 as a potent and essential regulator of the host response to SARS-CoV-2 infection and highlight the potential of BRD2 as a therapeutic target for COVID-19. 2022-01 2022-01-13 /pmc/articles/PMC8820466/ /pubmed/35027731 http://dx.doi.org/10.1038/s41556-021-00821-8 Text en Users may view, print, copy, and download text and data-mine the content in such documents, for the purposes of academic research, subject always to the full Conditions of use: https://www.springernature.com/gp/open-research/policies/accepted-manuscript-terms |
spellingShingle | Article Samelson, Avi J. Tran, Quang Dinh Robinot, Rémy Carrau, Lucia Rezelj, Veronica V. Kain, Alice Mac Chen, Merissa Ramadoss, Gokul N. Guo, Xiaoyan Lim, Shion A. Lui, Irene Nuñez, James K. Rockwood, Sarah J. Wang, Jianhui Liu, Na Carlson-Stevermer, Jared Oki, Jennifer Maures, Travis Holden, Kevin Weissman, Jonathan S. Wells, James A. Conklin, Bruce R. TenOever, Benjamin R. Chakrabarti, Lisa A. Vignuzzi, Marco Tian, Ruilin Kampmann, Martin BRD2 inhibition blocks SARS-CoV-2 infection by reducing transcription of the host cell receptor ACE2 |
title | BRD2 inhibition blocks SARS-CoV-2 infection by reducing transcription of the host cell receptor ACE2 |
title_full | BRD2 inhibition blocks SARS-CoV-2 infection by reducing transcription of the host cell receptor ACE2 |
title_fullStr | BRD2 inhibition blocks SARS-CoV-2 infection by reducing transcription of the host cell receptor ACE2 |
title_full_unstemmed | BRD2 inhibition blocks SARS-CoV-2 infection by reducing transcription of the host cell receptor ACE2 |
title_short | BRD2 inhibition blocks SARS-CoV-2 infection by reducing transcription of the host cell receptor ACE2 |
title_sort | brd2 inhibition blocks sars-cov-2 infection by reducing transcription of the host cell receptor ace2 |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8820466/ https://www.ncbi.nlm.nih.gov/pubmed/35027731 http://dx.doi.org/10.1038/s41556-021-00821-8 |
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