The Transmembrane Protease TMPRSS2 as a Therapeutic Target for COVID-19 TreatmentReview Published on 2022-01-252022-10-29 Journal: International Journal of Molecular Sciences [Category] COVID-19, SARS, [키워드] clinical development cofactor coronavirus COVID-19 epithelial cell expression gastrointestinal tract glycoprotein Influenza inhibiting other organs other respiratory virus physiological Prostate protease Protease inhibitor respiratory viruses SARS-CoV-2 SARS-CoV-2 entry substrate target TMPRSS2 TMPRSS2 inhibitor transmembrane Treatment viral infection [DOI] 10.3390/ijms23031351 PMC 바로가기 [Article Type] Review
Hydroxychloroquine treatment on SARS-CoV-2 receptor ACE2, TMPRSS2 and NRP1 expression in human primary pterygium and conjunctival cells인간의 일차 익상편 및 결막 세포에서 SARS-CoV-2 수용체 ACE2, TMPRSS2 및 NRP1 발현에 대한 히드록시클로로퀸 치료Multicenter Study Published on 2022-01-012022-09-11 Journal: Experimental eye research [Category] SARS, 바이오마커, [키워드] ACE2 ACE2 protein acute respiratory syndrome acute respiratory syndrome coronavirus angiotensin Angiotensin-converting enzyme angiotensin-converting enzyme 2 applied binding Cell cell viability cells Combination concentration of hydroxychloroquine Conjunctiva conjunctival coronavirus coronavirus disease Coronavirus disease 2019 COVID-19 COVID-19 treatment decrease elevated enzyme epithelial evaluate expression fibroblasts host cell host cell receptor Hydroxychloroquine hydroxychloroquine treatment increase in Infection influences neuropilin Neuropilin-1 NRP1 oxidative stress pandemic pathogen Protein protein expression Pterygium reduced reduction respiratory ROS production SARS-CoV-2 SARS-CoV-2 receptor Serine severe acute respiratory syndrome Coronavirus severe acute respiratory syndrome coronavirus 2 Side effect significantly SOD2 Spike protein tissue TMPRSS2 TMPRSS2 expression TMPRSS2 inhibitor TMPRSS2 protein TMPRSS2. transmembrane serine protease Treatment Treatment strategies type II transmembrane serine protease viability [DOI] 10.1016/j.exer.2021.108864 PMC 바로가기 [Article Type] Multicenter Study
A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells새로운 종류의 TMPRSS2 억제제는 SARS-CoV-2 및 MERS-CoV 바이러스 진입을 강력하게 차단하고 인간 상피 폐 세포를 보호합니다410 Published on 2021-10-112022-09-10 Journal: Proceedings of the National Academy of Sciences of [Category] MERS, SARS, 신약개발, [키워드] activate acute respiratory syndrome acute respiratory syndrome coronavirus acute respiratory syndrome coronavirus 2 addition Antiviral antiviral drug block broad-spectrum antivirals Calu Calu-3 calu-3 cells camostat can be used cell entry chimeric clinical development coronavirus COVID-19 COVID-19 treatment Cytopathic effect cytopathic effects drug drug candidate drug design Drug discovery drugs Efficacy epithelial epithelial cell epithelial cells full-length half-life half-maximal effective concentration half-maximal inhibitory concentration help host cell human lung in vivo Influenza influenza viruses inhibiting inhibitor lead lung lung cell lung tissue mechanism MERS-CoV mice Middle East Middle East respiratory syndrome Middle East respiratory syndrome Coronavirus nafamostat other coronavirus other coronaviruses Pathogenesis pharmacokinetics plasma probe protease Protease inhibitor PROTECT Protein PS-SCL respiratory respiratory syndrome coronavirus SARS-CoV SARS-CoV-2 SARS-COV-2 infection SARS-CoV-2 infections SARS-CoV-2 virus selective Serine serine protease TMPRSS2 severe acute respiratory syndrome Coronavirus Significance significantly specificity Spike protein stability structure-based drug discovery the Spike therapeutic target TMPRSS2 TMPRSS2 inhibitor TMPRSS2 inhibitors TMPRSS2 protein treat Treatment Viral viral entry viral pathogenesis Viral protein viral spread virus [DOI] 10.1073/pnas.2108728118 PMC 바로가기 [Article Type] 410
A phase I study of high dose camostat mesylate in healthy adults provides a rationale to repurpose the TMPRSS2 inhibitor for the treatment of COVID-19건강한 성인을 대상으로 한 고용량 카모스타트 메실레이트에 대한 1상 연구는 COVID-19 치료를 위해 TMPRSS2 억제제를 용도 변경하는 근거를 제공합니다Clinical Trial Published on 2021-09-012022-09-11 Journal: Clinical and translational science [Category] 신약개발, 임상, [키워드] acute respiratory syndrome acute respiratory syndrome coronavirus acute respiratory syndrome coronavirus 2 addition Administered camostat Camostat mesylate Cell chronic pancreatitis Concentration conducted coronavirus coronavirus disease Coronavirus disease 2019 COVID-19 dosages effective evaluated half-maximal effective concentration healthy High dose High-dose Infection inhibit inhibiting meal metabolite no significant difference Pancreatitis Phase I Phenylacetic acid plasma provide reflux esophagitis reported respiratory Safe safety profile Serine serine protease inhibitor severe acute respiratory syndrome Coronavirus significantly Simulation TMPRSS2 inhibitor transmembrane serine protease treat Treatment type II transmembrane serine protease [DOI] 10.1111/cts.13052 PMC 바로가기 [Article Type] Clinical Trial
Hesperidin Is a Potential Inhibitor against SARS-CoV-2 Infection헤스페리딘은 SARS-CoV-2 감염에 대한 잠재적 억제제입니다Article Published on 2021-08-162022-09-10 Journal: Nutrients [Category] MERS, SARS, 변종, [키워드] 501Y.V2 ACE2 acute respiratory syndrome acute respiratory syndrome coronavirus acute respiratory syndrome coronavirus 2 aglycone angiotensin Angiotensin-converting enzyme angiotensin-converting enzyme 2 Bioavailability cellular cellular entry cellular receptor coronavirus D614G docking hesperetin hesperidin Infection Interaction metabolite Particles Potential Proteins reducing reduction required respiratory S protein SARS-CoV-2 SARS-COV-2 infection Serine severe acute respiratory syndrome Coronavirus shown suppressed the S protein the SARS-CoV-2 TMPRSS2 TMPRSS2 expression TMPRSS2 inhibitor transmembrane serine protease transmembrane serine protease 2 variants variants of SARS-CoV-2 VeroE6 cell VeroE6 cells wild type [DOI] 10.3390/nu13082800 PMC 바로가기 [Article Type] Article
Identification of 13 Guanidinobenzoyl- or Aminidinobenzoyl-Containing Drugs to Potentially Inhibit TMPRSS2 for COVID-19 TreatmentArticle Published on 2021-06-302022-10-29 Journal: International Journal of Molecular Sciences [Category] COVID-19, MERS, [키워드] addition Analysis approved arginine assumption binding interaction camostat catalytic domain clinically compounds Coronaviruses COVID-19 docking drug drugs effective group groups hallmark high stability identification inhibit Interaction involved lysine molecular molecular dynamics Molecular dynamics simulation nafamostat Salt Bridge SARS-CoV-2 serine protease TMPRSS2 Spread suggested supported TMPRSS2 TMPRSS2 inhibitor Treatment trypsin viral entry [DOI] 10.3390/ijms22137060 PMC 바로가기 [Article Type] Article
Alpha 1 Antitrypsin is an Inhibitor of the SARS-CoV-2–Priming Protease TMPRSS2Research Article Published on 2021-04-262022-10-28 Journal: Pathogens and Immunity [Category] COVID-19, [키워드] ACE2 affecting Alpha Alpha 1 antitrypsin angiotensin-converting enzyme 2 antitrypsin binding Camostat mesylate cell entry Complexes coronavirus coronavirus S protein Coronaviruses COVID disease severity dissemination docked domain effective Extracellular FDA-approved drug host cells identify implicated Infection membrane MERS plasma priming protease receptor SARS CoV-2 SARS-CoV SARS-CoV-2 SARS-CoV-2 viral load serine protease serine protease inhibitor suggested Support the S protein TMPRSS2 TMPRSS2 inhibitor TMPRSS2 inhibitors Treatment with COVID-19 [DOI] 10.20411/pai.v6i1.408 PMC 바로가기 [Article Type] Research Article
Efficacy of the TMPRSS2 inhibitor camostat mesilate in patients hospitalized with Covid-19-a double-blind randomized controlled trial.Research article Published on 2021-04-222022-10-05 Journal: EClinicalMedicine [Category] 임상, [키워드] 30-Day mortality 7-point ordinal scale 95% confidence interval acute respiratory syndrome Admission adverse event assigned baseline camostat mesilate cell entry Clinical improvement conducted coronavirus coronavirus disease discharge double-blind EudraCT evaluated finding Frequency hazard ratio Hospitalization ICU admission in viral Infection interquartile range investigator-initiated IQR Mortality Multicenter trial not affect Oropharyngeal Other outcome participant Patient patients hospitalized Placebo placebo-controlled Primary outcome progression protease protocol Randomized Randomized controlled trial randomized trials Randomly receive SARS-CoV-2 SARS-COV-2 infection serine 2 the placebo group TMPRSS2 TMPRSS2 inhibitor Treatment two groups Viral load [DOI] 10.1016/j.eclinm.2021.100849 [Article Type] Research article
Cross-linking peptide and repurposed drugs inhibit both entry pathways of SARS-CoV-2가교 펩타이드 및 용도 변경 약물은 SARS-CoV-2의 두 진입 경로를 모두 억제합니다Article Published on 2021-03-092022-08-31 Journal: Nature Communications [Category] SARS, 신약개발, 치료제, [키워드] Antiviral approach Arbidol camostat cells Chloroquine cocktail Combination coronavirus Coronaviruses COVID-19 COVID-19 treatment Cross-linking drug combination Drug discovery effective Endocytic pathway Endosomal acidification ENhance entry pathway hamster hamsters identify in vitro in vivo inhibit inhibit SARS-CoV-2 inhibiting inhibitor mice pathway peptide Repurposed drug Repurposed drugs SARS-CoV SARS-CoV-2 SARS-CoV-2 replication SARS-CoV-2 virus significantly suppress suppresse therapy TMPRSS2 TMPRSS2 inhibitor today treating COVID-19 Treatment treatment trial treatment trials umifenovir Viral viral replication virus entry [DOI] 10.1038/s41467-021-21825-w PMC 바로가기 [Article Type] Article
Hydroxychloroquine-mediated inhibition of SARS-CoV-2 entry is attenuated by TMPRSS2SARS-CoV-2 진입의 Hydroxychloroquine 매개 억제는 TMPRSS2에 의해 약화됩니다Research Article Published on 2021-01-192022-08-13 Journal: PLoS Pathogens [Category] COVID-19, Medicine and Health Sciences, [키워드] ablated activate activated activating antiviral activities antiviral activity Autoimmune disorders block cathepsin L Cathepsins cause Cell cell entry cell surface cell-culture studies cell-culture systems Chloroquine cleave clinically Combination combinations coronavirus COVID-19 COVID-19 patient dependent on Efficacy endocytosis Endosomal acidification endosomal protease explain functional furin furin cleavage site furin-cleavage site global public health human clinical trial human clinical trials Hydroxychloroquine identify in vivo Infection inhibit inhibit SARS-CoV-2 interfere introduced lack malaria membrane fusion observé pathogenic coronavirus pathway plasma plasma membrane Prevent protease TMPRSS2 Protein Proteins proteolytic activity Receptor binding reversed S protein S proteins SARS Coronavirus SARS-CoV-1 SARS-CoV-1 and -2 SARS-CoV-2 SARS-CoV-2 entry SARS-COV-2 infection SARS-CoV-2 S protein SARS-CoV-2 spike shown target cell target cells tested the cell the SARS-CoV-2 these compounds TMPRSS2 TMPRSS2 expression TMPRSS2 inhibitor TMPRSS2 pathway treat treated treatment for COVID-19 utility Viral viral entry viral infection [DOI] 10.1371/journal.ppat.1009212 PMC 바로가기 [Article Type] Research Article