The DOI matches its Crossref record; 32 of the 32 references it cites were found in a registry or an index.
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19
Open accessAbstract
Abstract The novel coronavirus disease COVID-19 that emerged in 2019 is caused by the virus SARS CoV-2 and named for its close genetic similarity to SARS CoV-1 that caused severe acute respiratory syndrome (SARS) in 2002. Both SARS coronavirus genomes encode two overlapping large polyproteins, which are cleaved at specific sites by a 3C-like cysteine protease (3CLpro) in a post-translational processing step that is critical for coronavirus replication. The 3CLpro sequences for CoV-1 and CoV-2 viruses are 100% identical in the catalytic domain that carries out protein cleavage. A research effort that focused on the discovery of reversible and irreversible ketone-based inhibitors of SARS CoV-1 3CLpro employing ligand-protease structures solved by X-ray crystallography led to the identification of 3 and 4. Preclinical experiments reveal 4 (PF-00835231) as a potent inhibitor of CoV-2 3CLpro with suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.
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Cites
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An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19
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Self-citationAdvances in covalent drug discovery
Boike, L., Henning, N. J., & Nomura, D. K. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-022-00542-z · Cited by 823
Therapeutic strategies for COVID-19: progress and lessons learned
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Use of molecular docking computational tools in drug discovery
(2021) · Progress in Medicinal Chemistry · doi:10.1016/bs.pmch.2021.01.004 · Cited by 621
SARS-CoV-2 M pro inhibitors with antiviral activity in a transgenic mouse model
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Metadata
- Authors
- Hoffman, R. L., Kania, R. S., Brothers, M. A., Davies, J. F., Ferre, R. A., Gajiwala, K. S., He, M., Hogan, R. J., Kozminski, K., Li, L. Y., Lockner, J. W., Lou, J., Marra, M. T., Mitchell, L. J., Murray, B. W., Nieman, J. A., Noell, S., Planken, S. P., Rowe, T., Ryan, K., Smith, G. J., Solowiej, J. E., Steppan, C. M., & Taggart, B.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2020-10-15
- Volume
- 63
- Issue
- 21
- Pages
- 12725-12747
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W3090894484
- Cited by
- 507
- References
- 32
- FWCI
- 10.56
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Hoffman, R. L., Kania, R. S., Brothers, M. A., Davies, J. F., Ferre, R. A., Gajiwala, K. S., He, M., Hogan, R. J., Kozminski, K., Li, L. Y., Lockner, J. W., Lou, J., Marra, M. T., Mitchell, L. J., Murray, B. W., Nieman, J. A., Noell, S., Planken, S. P., Rowe, T., . . . Taggart, B. (2020). Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.0c01063
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
