The DOI matches its Crossref record; 63 of the 63 references it cites were found in a registry or an index.
Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19
Open accessAbstract
COVID-19 caused by the SARS-CoV-2 virus has become a global pandemic. 3CL protease is a virally encoded protein that is essential across a broad spectrum of coronaviruses with no close human analogs. PF-00835231, a 3CL protease inhibitor, has exhibited potent in vitro antiviral activity against SARS-CoV-2 as a single agent. Here we report, the design and characterization of a phosphate prodrug PF-07304814 to enable the delivery and projected sustained systemic exposure in human of PF-00835231 to inhibit coronavirus family 3CL protease activity with selectivity over human host protease targets. Furthermore, we show that PF-00835231 has additive/synergistic activity in combination with remdesivir. We present the ADME, safety, in vitro, and in vivo antiviral activity data that supports the clinical evaluation of PF-07304814 as a potential COVID-19 treatment.
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Cited by
Naturally Occurring Mutations of SARS-CoV-2 Main Protease Confer Drug Resistance to Nirmatrelvir
Hu, Y., Lewandowski, E. M., Tan, H., Zhang, X., Morgan, R. T., Zhang, X., Jacobs, L. M. C., Butler, S. G., Gongora, M. V., Choy, J., et al. (2023) · ACS Central Science · doi:10.1021/acscentsci.3c00538 · Cited by 333
Self-citationA critical overview of computational approaches employed for COVID-19 drug discovery
Muratov, E. N., Amaro, R., Andrade, C. H., Brown, N., Ekins, S., Fourches, D., Isayev, O., Kozakov, D., Medina-Franco, J. L., Merz, K. M., et al. (2021) · Chemical Society Reviews · doi:10.1039/d0cs01065k · Cited by 206
Metadata
- Authors
- Boras, B., Jones, R. M., Anson, B. J., Arenson, D., Aschenbrenner, L., Bakowski, M. A., Beutler, N., Binder, J., Chen, E., Eng, H., Hammond, H., Hammond, J., Haupt, R. E., Hoffman, R., Kadar, E. P., Kania, R., Kimoto, E., Kirkpatrick, M. G., Lanyon, L., Lendy, E. K., Lillis, J. R., Logue, J., Luthra, S. A., Ma, C., Mason, S. W., McGrath, M. E., Noell, S., Obach, R. S., O’ Brien, M. N., O’Connor, R., Ogilvie, K., Owen, D., Pettersson, M., Reese, M. R., Rogers, T. F., Rosales, R., Rossulek, M. I., Sathish, J. G., Shirai, N., Steppan, C., Ticehurst, M., Updyke, L. W., Weston, S., Zhu, Y., White, K. M., García-Sastre, A., Wang, J., Chatterjee, A. K., Mesecar, A. D., Frieman, M. B., Anderson, A. S., & Allerton, C.
- Venue
- Nature Communications
- Published
- 2021-10-18
- Volume
- 12
- Issue
- 1
- Pages
- 6055-6055
- ISSN
- 2041-1723 (ISSN-L)
- OpenAlex
- W3205127490
- Cited by
- 280
- References
- 63
- FWCI
- 17.99
- Type
- journal article
- Language
- en
- Open access
- gold
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- Boras, B., Jones, R. M., Anson, B. J., Arenson, D., Aschenbrenner, L., Bakowski, M. A., Beutler, N., Binder, J., Chen, E., Eng, H., Hammond, H., Hammond, J., Haupt, R. E., Hoffman, R., Kadar, E. P., Kania, R., Kimoto, E., Kirkpatrick, M. G., Lanyon, L., . . . Allerton, C. (2021). Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19. Nature Communications. https://doi.org/10.1038/s41467-021-26239-2
Data sources
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.
