Journal
MICROORGANISMS
Volume 9, Issue 4, Pages -Publisher
MDPI
DOI: 10.3390/microorganisms9040756
Keywords
SARS-CoV-2 3CL protease; drug repurposing; antiviral; FRET; inhibitory compounds
Categories
Funding
- Basic Science Research Programs - National Research Foundation of Korea - Ministry of Education, Science and Technology, Republic of Korea (MEST) [2018R1D1A1B07050781, 2018R1D1A1B07050942]
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The outbreak of COVID-19 caused chaos worldwide, leading to the urgent need for treatments. Drug-repurposing approach is a rapid strategy in developing treatments for COVID-19. Research showed that certain antiviral agents and phosphodiesterase type 5 inhibitors demonstrated good inhibitory effects on the protease function of the virus.
The outbreak of coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), results in serious chaos all over the world. In addition to the available vaccines, the development of treatments to cure COVID-19 should be done quickly. One of the fastest strategies is to use a drug-repurposing approach. To provide COVID-19 patients with useful information about medicines currently being used in clinical trials, twenty-four compounds, including antiviral agents, were selected and assayed. These compounds were applied to verify the inhibitory activity for the protein function of 3CLpros (main proteases) of SARS-CoV and SARS-CoV-2. Among them, viral reverse-transcriptase inhibitors abacavir and tenofovir revealed a good inhibitory effect on both 3CLpros. Intriguingly, sildenafil, a cGMP-specific phosphodiesterase type 5 inhibitor also showed significant inhibitory function against them. The in silico docking study suggests that the active-site residues located in the S1 and S2 sites play key roles in the interactions with the inhibitors. The result indicates that 3CLpros are promising targets to cope with SAR-CoV-2 and its variants. The information can be helpful to design treatments to cure patients with COVID-19.
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