Main protease mutants of SARS-CoV-2 variants remain susceptible to nirmatrelvir

S Ullrich, KB Ekanayake, G Otting, C Nitsche - Bioorganic & Medicinal …, 2022 - Elsevier
protease by disrupting the M pro dimer. The present study assesses the M pro mutants of
emerging SARS-CoV… We analyzed the most widespread amino acid substitutions in SARS-CoV-…

Naturally occurring mutations of SARS-CoV-2 main protease confer drug resistance to nirmatrelvir

Y Hu, EM Lewandowski, H Tan, X Zhang… - ACS central …, 2023 - ACS Publications
… The emergence of SARS-CoV-2 variants with mutations in M pro raised the alarm of … -resistant
mutants, we systematically characterized 102 naturally occurring M pro mutants located at …

[HTML][HTML] Ensitrelvir is effective against SARS-CoV-2 3CL protease mutants circulating globally

S Kawashima, Y Matsui, T Adachi, Y Morikawa… - Biochemical and …, 2023 - Elsevier
… m /V max of SARS-CoV-2 3CL pro mutants, proteolytic reactions were … SARS-CoV-2 3CL
pro mutants were used as an enzyme source and the synthesized peptide between SARS-CoV-…

Proteolytic activation of SARSCoV‐2 spike protein

M Takeda - Microbiology and immunology, 2022 - Wiley Online Library
… distinguishing features of SARS-CoV-2, and some of the characteristics of the mutant viruses
seem … Changes in cleavage properties and the proteases available for cleavage can cause …

[HTML][HTML] Global prevalence of SARS-CoV-2 3CL protease mutations associated with nirmatrelvir or ensitrelvir resistance

JD Ip, AWH Chu, WM Chan, RCY Leung… - …, 2023 - thelancet.com
… We compiled a list of 3CL pro mutations which have been associated with nirmatrelvir or
ensitrelvir … We analyzed the prevalence for different time periods, SARS-CoV-2 lineages and …

Evaluation of the Inhibition Potency of Nirmatrelvir against Main Protease Mutants of SARS-CoV-2 Variants

H Jiang, Y Zhou, X Zou, X Hu, J Wang, P Zeng, W Li… - Biochemistry, 2023 - ACS Publications
… further investigation on the mutants of SARS-CoV-2 M pro … mutants from SARS-CoV-2
variants and analyzed their susceptibility to inhibition by nirmatrelvir. These documented mutations

SARS-CoV-2 main protease drug design, assay development, and drug resistance studies

B Tan, R Joyce, H Tan, Y Hu… - Accounts of chemical …, 2022 - ACS Publications
… interaction of paxlovid, and the emergence of SARS-CoV-2 variants with potential drug-resistant
mutations, there is a pressing need for additional antivirals to combat current and future …

[HTML][HTML] Multiple pathways for SARS-CoV-2 resistance to nirmatrelvir

S Iketani, H Mohri, B Culbertson, SJ Hong, Y Duan… - Nature, 2023 - nature.com
… a multitude of 3CL protease mutations. In the experiment … lineages were selected with
mutations observed at 23 different … the mutations identified in this study with clinical SARS-CoV-…

[HTML][HTML] Potential resistance of SARS-CoV-2 main protease (Mpro) against protease inhibitors: lessons learned from HIV-1 protease

JA Mótyán, M Mahdi, G Hoffka, J Tőzsér - International journal of …, 2022 - mdpi.com
… Despite the comparable efficacy of nirmatrelvir against the wild-type protease and its point
mutants or variants in different virus strains, currently, we only have information about the PI-…

[PDF][PDF] D614G mutation alters SARS-CoV-2 spike conformation and enhances protease cleavage at the S1/S2 junction

SMC Gobeil, K Janowska, S McDowell, K Mansouri… - Cell reports, 2021 - cell.com
… study that the D614G mutation enhances susceptibility of the SARS-CoV-2 S … SARS-CoV-2
S D614G mutation on S structure, focusing on RBD conformation and changes in proteolytic