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Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Antimicrob+Agents+Chemother 2021 ; 65 (4): ä Nephropedia Template TP
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Kinetic Characterization and Inhibitor Screening for the Proteases Leading to Identification of Drugs against SARS-CoV-2 #MMPMID33526482
Kuo CJ; Chao TL; Kao HC; Tsai YM; Liu YK; Wang LH; Hsieh MC; Chang SY; Liang PH
Antimicrob Agents Chemother 2021[Mar]; 65 (4): ä PMID33526482show ga
Coronavirus (CoV) disease 2019 (COVID-19), caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has claimed many lives worldwide and is still spreading since December 2019. The 3C-like protease (3CL(pro)) and papain-like protease (PL(pro)) are essential for maturation of viral polyproteins in SARS-CoV-2 life cycle and thus regarded as key drug targets for the disease. In this study, 3CL(pro) and PL(pro) assay platforms were established, and their substrate specificities were characterized. The assays were used to screen collections of 1,068 and 2,701 FDA-approved drugs. After excluding the externally used drugs which are too toxic, we totally identified 12 drugs as 3CL(pro) inhibitors and 36 drugs as PL(pro) inhibitors active at 10 muM. Among these inhibitors, six drugs were found to suppress SARS-CoV-2 with the half-maximal effective concentration (EC(50)) below or close to 10 muM. This study enhances our understanding on the proteases and provides FDA-approved drugs for prevention and/or treatment of COVID-19.