Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activity
Sign Up to like & getrecommendations! Published in 2021 at "EBioMedicine"
DOI: 10.1016/j.ebiom.2021.103255
Abstract: Background Antivirals are needed to combat the COVID-19 pandemic, which is caused by SARS-CoV-2. The clinically-proven protease inhibitor Camostat mesylate inhibits SARS-CoV-2 infection by blocking the virus-activating host cell protease TMPRSS2. However, antiviral activity of… read more here.
Keywords: antiviral activity; tmprss2; camostat mesylate; mesylate ... See more keywords
Structure-based drug repositioning over the human TMPRSS2 protease domain: search for chemical probes able to repress SARS-CoV-2 Spike protein cleavages
Sign Up to like & getrecommendations! Published in 2020 at "European Journal of Pharmaceutical Sciences"
DOI: 10.1016/j.ejps.2020.105495
Abstract: Abstract In December 2019, a new coronavirus was identified in the Hubei province of central china and named SARS-CoV-2. This new virus induces COVID-19, a severe respiratory disease with high death rate. A putative target… read more here.
Keywords: protease; tmprss2; structure; sars cov ... See more keywords
Identification of novel TMPRSS2 inhibitors for COVID-19 using e-pharmacophore modelling, molecular docking, molecular dynamics and quantum mechanics studies
Sign Up to like & getrecommendations! Published in 2021 at "Informatics in Medicine Unlocked"
DOI: 10.1016/j.imu.2021.100758
Abstract: SARS coronavirus 2 has spread rapidly around the world and continues to have a massive global health effect, contributing to an infectious respiratory illness called coronavirus infection-19 (COVID-19). TMPRSS2 is an emerging molecular target that… read more here.
Keywords: pharmacophore; tmprss2; using pharmacophore; identification novel ... See more keywords
Discovery of novel TMPRSS2 inhibitors for COVID-19 using in silico fragment-based drug design, molecular docking, molecular dynamics, and quantum mechanics studies
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DOI: 10.1016/j.imu.2022.100870
Abstract: The global expansion of COVID-19 and the mutations of severe acute respiratory syndrome coronavirus necessitate quick development of treatment and vaccination. Because the androgen-responsive serine protease TMPRSS2 is involved in cleaving the SARS-CoV-2 spike protein… read more here.
Keywords: tmprss2; mechanics; fragment based; drug design ... See more keywords
Renin-angiotensin system blockade on angiotensin-converting enzyme 2 and TMPRSS2 in human type II pneumocytes
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DOI: 10.1016/j.lfs.2022.120324
Abstract: Aims Angiotensin-converting enzyme (ACE) 2 is the receptor for severe acute respiratory syndrome coronavirus 2 which causes coronavirus disease 2019 (COVID-19). Viral cellular entry requires ACE2 and transmembrane protease serine 2 (TMPRSS2). ACE inhibitors (ACEIs)… read more here.
Keywords: acei arb; tmprss2; arb treated; type pneumocytes ... See more keywords
Genetic association of TMPRSS2 rs2070788 polymorphism with COVID-19 case fatality rate among Indian populations
Sign Up to like & getrecommendations! Published in 2022 at "Infection, Genetics and Evolution"
DOI: 10.1016/j.meegid.2022.105206
Abstract: SARS-CoV2, the causative agent for COVID-19, an ongoing pandemic, engages the ACE2 receptor to enter the host cell through S protein priming by a serine protease, TMPRSS2. Variation in the TMPRSS2 gene may account for… read more here.
Keywords: tmprss2; tmprss2 gene; gene; rs2070788 ... See more keywords
ACE2 Receptor and TMPRSS2 Protein Expression Patterns in the Human Brainstem Reveal Anatomical Regions Potentially Vulnerable to SARS-CoV-2 Infection
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DOI: 10.1021/acschemneuro.3c00101
Abstract: Angiotensin-converting enzyme 2 receptor (ACE2R) is a transmembrane protein expressed in various tissues throughout the body that plays a key role in the regulation of blood pressure. Recently, ACE2R has gained significant attention due to… read more here.
Keywords: brainstem; expression; sars cov; tmprss2 ... See more keywords
ACE inhibition and cardiometabolic risk factors, lung ACE2 and TMPRSS2 gene expression, and plasma ACE2 levels: a Mendelian randomization study
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DOI: 10.1098/rsos.200958
Abstract: Angiotensin-converting enzyme 2 (ACE2) and serine protease TMPRSS2 have been implicated in cell entry for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the virus responsible for coronavirus disease 2019 (COVID-19). The expression of ACE2 and… read more here.
Keywords: tmprss2; lung ace2; ace2; expression ... See more keywords
Dual Inhibition of Vacuolar-ATPase and TMPRSS2 Is Required for Complete Blockade of SARS-CoV-2 Entry into Cells
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DOI: 10.1128/aac.00439-22
Abstract: An essential step in the infection life cycle of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the proteolytic activation of the viral spike (S) protein, which enables membrane fusion and entry into the… read more here.
Keywords: cell surface; entry; tmprss2; endosomal route ... See more keywords
Structural Basis of Covalent Inhibitory Mechanism of TMPRSS2-Related Serine Proteases by Camostat
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DOI: 10.1128/jvi.00861-21
Abstract: Serine proteases are a large family of enzymes critical for multiple physiological processes and proven diagnostic and therapeutic targets in several clinical indications. The serine protease transmembrane protease serine 2 (TMPRSS2) was recently found to… read more here.
Keywords: serine proteases; sars cov; camostat; protease ... See more keywords
TMPRSS2 Contributes to Virus Spread and Immunopathology in the Airways of Murine Models after Coronavirus Infection
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DOI: 10.1128/jvi.01815-18
Abstract: Broad-spectrum antiviral drugs against highly pathogenic coronaviruses and other emerging viruses are desirable to enable a rapid response to pandemic threats. Transmembrane protease serine type 2 (TMPRSS2), a protease belonging to the type II transmembrane… read more here.
Keywords: cov mers; immunopathology; mers cov; infection ... See more keywords