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A study of 3clpros as promising targets against sars-cov and sars-cov-2
- Title
- A study of 3clpros as promising targets against sars-cov and sars-cov-2
- Authors
- Jo S.; Kim S.; Yoo J.; Kim M.-S.; Shin D.H.
- Ewha Authors
- 신동해
- SCOPUS Author ID
- 신동해
- Issue Date
- 2021
- Journal Title
- Microorganisms
- ISSN
- 2076-2607
- Citation
- Microorganisms vol. 9, no. 4
- Keywords
- Antiviral; Drug repurposing; FRET; Inhibitory compounds; SARS-CoV-2 3CL protease
- Publisher
- MDPI AG
- Indexed
- SCIE; SCOPUS
- Document Type
- Article
- Abstract
- 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 com-pounds, 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. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.
- DOI
- 10.3390/microorganisms9040756
- Appears in Collections:
- 약학대학 > 약학과 > Journal papers
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