Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 36, Issue 1, Pages 147-153Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2020.1850710
Keywords
SARS-CoV-2 3CL protease; antiviral; repurposing drugs; FRET; 3CLpro inhibitors
Funding
- Ministry of Science and Technology, Taiwan [MOST 109-2327-B010-006]
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Researchers have identified several FDA-approved drugs that can effectively inhibit the proteolytic activity of SARS-CoV-2 virus, demonstrating their therapeutic potential for treating COVID-19 and other Betacoronavirus infections.
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is responsible for coronavirus disease 2019 (COVID-19). Since its emergence, the COVID-19 pandemic has not only distressed medical services but also caused economic upheavals, marking urgent the need for effective therapeutics. The experience of combating SARS-CoV and MERS-CoV has shown that inhibiting the 3-chymotrypsin-like protease (3CLpro) blocks the replication of the virus. Given the well-studied properties of FDA-approved drugs, identification of SARS-CoV-2 3CLpro inhibitors in an FDA-approved drug library would be of great therapeutic value. Here, we screened a library consisting of 774 FDA-approved drugs for potent SARS-CoV-2 3CLpro inhibitors, using an intramolecularly quenched fluorescence (IQF) peptide substrate. Ethacrynic acid, naproxen, allopurinol, butenafine hydrochloride, raloxifene hydrochloride, tranylcypromine hydrochloride, and saquinavir mesylate have been found to block the proteolytic activity of SARS-CoV-2 3CLpro. The inhibitory activity of these repurposing drugs against SARS-CoV-2 3CLpro highlights their therapeutic potential for treating COVID-19 and other Betacoronavirus infections.
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