Validation and invalidation of SARS-CoV-2 main protease inhibitors using the Flip-GFP and Protease-Glo luciferase assays
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Abstract
Abstract SARS-CoV-2 main protease (M pro ) is one of the most extensive exploited drug targets for COVID-19. Structurally disparate compounds have been reported as M pro inhibitors, raising the question of their target specificity. To elucidate the target specificity and the cellular target engagement of the claimed M pro inhibitors, we systematically characterize their mechanism of action using the cell-free FRET assay, the thermal shift-binding assay, the cell lysate Protease-Glo luciferase assay, and the cell-based Flip-GFP assay. Collectively, our results have shown that majority of the M pro inhibitors identified from drug repurposing including ebselen, carmofur, disulfiram, and shikonin are promiscuous cysteine inhibitors that are not specific to M pro , while chloroquine, oxytetracycline, montelukast, candesartan, and dipyridamole do not inhibit M pro in any of the assays tested. Overall, our study highlights the need of stringent hit validation at the early stage of drug discovery. Graphical abstract Flip-GFP and Protease-Glo luciferase assays, coupled with the FRET and thermal shift binding assays, were applied to validate the reported SARS-CoV-2 M pro inhibitors.
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The inhibitory potential of DIS on Mpro and PLpro was contradictory.
“Ultimately, the inhibitory potential of DIS on Mpro and PLpro was contradictory.98,99”
From Off-label and repurposed use of disulfiram beyond alcohol dependence: A systematic review of clinical and preclinical evidence (2026) · cites this paper as [98]
In Results and discussion, under “Bioactive compounds from drug repurposing” (page unavailable), the paper contrasts an earlier report that disulfiram inhibits Mpro with follow-up findings, including its own, that it did not inhibit Mpro under the tested conditions. It also reports proposed PLpro inhibition, but does not describe contradictory findings for PLpro. (LLM, conf=0.84)
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- Authors
- Ma, C., Tan, H., Choza, J., Wang, Y., & Wang, J.
- Affiliations
- University of Arizona (US)
- Corresponding author
- Wang, Jun
- Venue
- Acta Pharmaceutica Sinica B
- Publisher
- Elsevier BV
- Published
- 2022-04
- Volume
- 12
- Issue
- 4
- Pages
- 1636-1651
- ISSN
- 2211-3835 (ISSN-L)
- PMC
- PMC8558150
- OpenAlex
- W3208802464
- Cited by
- 86
- References
- 69
- Citations by year
- 2026: 5 · 2025: 16 · 2024: 16 · 2023: 21 · 2022: 25 · 2021: 3
- FWCI
- 5.31
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Acta Pharmaceutica Sinica B (publishedVersion, cc-by-nc-nd)
- bioRxiv (Cold Spring Harbor Laboratory) (acceptedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- National Institute of Allergy and Infectious Diseases (AI147325, AI157046, AI158775)
- University of Pennsylvania
- Topics
- Health Sciences › Medicine › Infectious Diseases › SARS-CoV-2 and COVID-19 Research
- Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
- Health Sciences › Medicine › Infectious Diseases › SARS-CoV-2 detection and testing
- Keywords
- main protease, Mpro inhibitors, COVID-19 drug repurposing, target specificity, hit validation, FRET assay, cysteine protease inhibitors, ebselen, carmofur, disulfiram, shikonin, chloroquine, oxytetracycline, montelukast, candesartan, dipyridamole
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