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Biochemical screening for SARS-CoV-2 main protease inhibitors
Camila Coelho1, Gloria Gallo1, Claudia B Campos1
1Department of Science and Technology, Federal University of São Paulo, São José dos Campos, Brazil.
Plos One
|October 6, 2020
Summary
Researchers screened compounds to find inhibitors of SARS-CoV-2
Area of Science:
- Virology
- Drug Discovery
- Biochemistry
Background:
- The Severe Acute Respiratory Syndrome Corona Virus 2 (SARS-CoV-2) pandemic poses a significant global health threat.
- Viral replication depends on non-structural proteins, including the main protease (Mpro), essential for processing viral polyproteins.
Purpose of the Study:
- To perform biochemical high-throughput screening (HTS) to identify inhibitors of the SARS-CoV-2 main protease (Mpro).
- To discover potential lead compounds for developing novel antiviral therapies against SARS-CoV-2.
Main Methods:
- Biochemical high-throughput screening (HTS) using a fluorescent assay.
- Utilized a compound library comprising known drugs, bioactive molecules, and natural products.
- Tested recombinantly expressed SARS-CoV-2 Mpro for inhibitory activity.
Main Results:
- Identified 13 inhibitors of SARS-CoV-2 Mpro with IC50 values between 0.2 μM and 23 μM.
- Confirmed known SARS-CoV Mpro inhibitors, including thimerosal and phenylmercuric acetate, as effective against SARS-CoV-2 Mpro.
- Discovered benzophenone derivatives and Evans blue as potent Mpro inhibitors.
Conclusions:
- The identified compounds, including benzophenone derivatives and Evans blue, show promise as starting points for SARS-CoV-2 drug development.
- This study provides valuable insights into potential therapeutic strategies targeting viral proteases.
