An Enzymatic TMPRSS2 Assay for Assessment of Clinical Candidates and Discovery of Inhibitors as Potential Treatment of COVID-19
Jonathan H. Shrimp, Stephen C. Kales, Philip E.J. Sanderson, Anton Simeonov, Min Shen, Matthew D. Hall
Abstract
= 130 nM). Bromhexine hydrochloride showed no inhibition of TMPRSS2. Further profiling of camostat, nafamostat, and gabexate against a panel of recombinant proteases provides insight into selectivity and potency.
Topics & Concepts
TMPRSS2ProteasesPharmacologyIC50Protease inhibitor (pharmacology)Viral entryChemistryVirologyBiologyVirusEnzymeViral loadCoronavirus disease 2019 (COVID-19)MedicineBiochemistryIn vitroViral replicationInfectious disease (medical specialty)DiseasePathologyAntiretroviral therapySARS-CoV-2 and COVID-19 ResearchComputational Drug Discovery MethodsMosquito-borne diseases and control