A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells Article Swipe
Matthew Mahoney
,
Vishnu C. Damalanka
,
Michael A. Tartell
,
Dong hee Chung
,
André Luiz Lourenço
,
Dustin Pwee
,
Anne E. Mayer Bridwell
,
Markus Hoffmann
,
Jorine Voss
,
Partha Karmakar
,
Nurit P. Azouz
,
Andrea M. Klingler
,
Paul W. Rothlauf
,
Cassandra E. Thompson
,
Melody Lee
,
Lidija Klampfer
,
Christina L. Stallings
,
Marc E. Rothenberg
,
Stefan Pöhlmann
,
Sean P. J. Whelan
,
Anthony J. O’Donoghue
,
Charles S. Craik
,
James W. Janetka
·
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.1073/pnas.2108728118
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.1073/pnas.2108728118
Significance MM3122 represents an advanced lead candidate for clinical development as a novel antiviral drug for COVID-19. In addition to being novel drugs, these selective TMRSS2 inhibitors can be used as valuable chemical probes to help elucidate mechanisms of viral pathogenesis. Since TMPRSS2 plays a key role as a viral protein processing protease in the pathogenesis of other coronaviruses (SARS-CoV, MERS-CoV) as well as influenza viruses, MM3122 and this class of TMPRSS2 inhibitors hold much promise as new drugs to not only treat SARS-CoV-2 infections but also potentially represent broad-spectrum antivirals.
Related Topics
Concepts
TMPRSS2
Virology
Serine protease
Ex vivo
Coronavirus
Virus
Proteases
In vivo
Viral entry
Protease
Protease inhibitor (pharmacology)
Cytopathic effect
Biology
Viral replication
Viral load
Coronavirus disease 2019 (COVID-19)
Medicine
Enzyme
Biochemistry
Disease
Infectious disease (medical specialty)
Biotechnology
Pathology
Antiretroviral therapy
Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.1073/pnas.2108728118
- https://www.pnas.org/doi/pdf/10.1073/pnas.2108728118
- OA Status
- hybrid
- Cited By
- 106
- References
- 65
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W3205193484
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W3205193484Canonical identifier for this work in OpenAlex
- DOI
-
https://doi.org/10.1073/pnas.2108728118Digital Object Identifier
- Title
-
A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cellsWork title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
-
2021Year of publication
- Publication date
-
2021-10-11Full publication date if available
- Authors
-
Matthew Mahoney, Vishnu C. Damalanka, Michael A. Tartell, Dong hee Chung, André Luiz Lourenço, Dustin Pwee, Anne E. Mayer Bridwell, Markus Hoffmann, Jorine Voss, Partha Karmakar, Nurit P. Azouz, Andrea M. Klingler, Paul W. Rothlauf, Cassandra E. Thompson, Melody Lee, Lidija Klampfer, Christina L. Stallings, Marc E. Rothenberg, Stefan Pöhlmann, Sean P. J. Whelan, Anthony J. O’Donoghue, Charles S. Craik, James W. JanetkaList of authors in order
- Landing page
-
https://doi.org/10.1073/pnas.2108728118Publisher landing page
- PDF URL
-
https://www.pnas.org/doi/pdf/10.1073/pnas.2108728118Direct link to full text PDF
- Open access
-
YesWhether a free full text is available
- OA status
-
hybridOpen access status per OpenAlex
- OA URL
-
https://www.pnas.org/doi/pdf/10.1073/pnas.2108728118Direct OA link when available
- Concepts
-
TMPRSS2, Virology, Serine protease, Ex vivo, Coronavirus, Virus, Proteases, In vivo, Viral entry, Protease, Protease inhibitor (pharmacology), Cytopathic effect, Biology, Viral replication, Viral load, Coronavirus disease 2019 (COVID-19), Medicine, Enzyme, Biochemistry, Disease, Infectious disease (medical specialty), Biotechnology, Pathology, Antiretroviral therapyTop concepts (fields/topics) attached by OpenAlex
- Cited by
-
106Total citation count in OpenAlex
- Citations by year (recent)
-
2025: 20, 2024: 31, 2023: 24, 2022: 28, 2021: 3Per-year citation counts (last 5 years)
- References (count)
-
65Number of works referenced by this work
- Related works (count)
-
10Other works algorithmically related by OpenAlex
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