B, expression of active WT protease or (C) the Q-1A mutant in the presence of the inhibitors nirmatrelvir (NMV) and ensitrelvir (ENS). preMpro, precursor form of Mpro; Mpro, main protease. The Q-1A mutant, purified using the nickel2+ ion that has been coupled to nitrilotriacetic ...
Such a profile was also observed for ensitrelvir, another clinically relevant Mpro inhibitor. These results shed light on the mechanisms by which SARS-CoV-2 evolves to develop resistance to the current generation of protease inhibitors and provide the basis for the design of next-generation Mpro...
ITR, adenovirus inverted terminal repeat; Pa, adenovirus packaging signal; CBA-P, chicken beta actin gene promoter with CVM enhancer; UbC-int, the first intron of the human ubiquitin C gene; SP, the human cystatin-S signal peptide; RBD, receptor binding domain of the SARS-CoV-2 spike ...
Molecular mechanism of ensitrelvir inhibiting SARS-CoV-2 main protease and its variants Commun. Biol., 6 (1) (Jul. 2023), p. 694, 10.1038/s42003-023-05071-y View PDFView articleGoogle Scholar [49] Y. Furuta, T. Komeno, T. Nakamura Favipiravir (T-705), a broad spectrum inhibitor ...
Previous research identified resistance of N142A or N142S variants against nirmatrelvir, GC376, and ensitrelvir [34, 35], which we presumed might be partly due to the improved enzymatic activity and unaffected stability of these Mpro mutants since no loss of interaction was observed. Other ...
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Ensitrelvir (formerly S-217622), as a potential treatment for SARS-CoV-2 has been reported [[106], [107], [108]]. Ensitrelvir demonstrates strong in vitro antiviral activity against the SARS-CoV-2 Omicron subvariants BA.4 and BA.5. As the world's first coronavirus oral drug approved...
Rhonda D. Cardin (Pfizer) for providing us with the solvate form of nirmatrelvir. This project has received funding from the Covid-19-Fund KU Leuven/UZ Leuven and the COVID-19 call of FWO (G0G4820N), the European Union’s Horizon 2020 research and innovation program under grant ...
Since most omicron subvariants have reduced sensitivity to most monoclonal antibody therapies, SARS-CoV-2 resistance to other antivirals including main protease inhibitors such as ensitrelvir is a major public health concern. Here, repeating passages of SARS-CoV-2 in the presence of ensitrelvir ...
Novel Investigational Anti-SARS-CoV-2 Agent Ensitrelvir “S-217622”: A Very Promising Potential Universal Broad-Spectrum Antiviral at the Therapeutic Frontline of Coronavirus Species 2023, ACS Omega Evaluation of a series of nucleoside analogs as effective anticoronaviral-2 drugs against the Omicron...