In vitro and in vivo characterization of SARS-CoV-2 resistance to ensitrelvir
M Kiso, S Yamayoshi, S Iida, Y Furusawa… - Nature …, 2023 - nature.com
Ensitrelvir, an oral antiviral agent that targets a SARS-CoV-2 main protease (3CLpro or
Nsp5), is clinically useful against SARS-CoV-2 including its omicron variants. Since most …
Nsp5), is clinically useful against SARS-CoV-2 including its omicron variants. Since most …
Development of de-novo coronavirus 3-chymotrypsin-like protease (3CLpro) inhibitors since COVID-19 outbreak: A strategy to tackle challenges of persistent virus …
L Tian, T Qiang, X Yang, Y Gao, X Zhai, K Kang… - European Journal of …, 2024 - Elsevier
Although no longer a public health emergency of international concern, COVID-19 remains
a persistent and critical health concern. The development of effective antiviral drugs could …
a persistent and critical health concern. The development of effective antiviral drugs could …
Inhibitors of SARS-CoV-2 main protease (Mpro) as anti-coronavirus agents
A Zagórska, A Czopek, M Fryc, J Jończyk - Biomolecules, 2024 - pmc.ncbi.nlm.nih.gov
The main protease (Mpro) of SARS-CoV-2 is an essential enzyme that plays a critical part in
the virus's life cycle, making it a significant target for developing antiviral drugs. The …
the virus's life cycle, making it a significant target for developing antiviral drugs. The …
An orally bioavailable SARS-CoV-2 main protease inhibitor exhibits improved affinity and reduced sensitivity to mutations
Inhibitors of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main
protease (Mpro) such as nirmatrelvir (NTV) and ensitrelvir (ETV) have proven effective in …
protease (Mpro) such as nirmatrelvir (NTV) and ensitrelvir (ETV) have proven effective in …
[HTML][HTML] Generation and evaluation of protease inhibitor-resistant SARS-CoV-2 strains
HS Bouzidi, JS Driouich, R Klitting, O Bernadin… - Antiviral Research, 2024 - Elsevier
Since the start of the SARS-CoV-2 pandemic, the search for antiviral therapies has been at
the forefront of medical research. To date, the 3CLpro inhibitor nirmatrelvir (Paxlovid®) has …
the forefront of medical research. To date, the 3CLpro inhibitor nirmatrelvir (Paxlovid®) has …
A Gaussia luciferase reporter assay for the evaluation of coronavirus Nsp5/3CLpro activity
A Vlachou, R Nchioua, K Regensburger, F Kirchhoff… - Scientific Reports, 2024 - nature.com
Human coronaviruses (hCoVs) infect millions of people every year. Among these, MERS,
SARS-CoV-1, and SARS-CoV-2 caused significant morbidity and mortality and their …
SARS-CoV-1, and SARS-CoV-2 caused significant morbidity and mortality and their …
Miniaturized Modular Click Chemistry‐enabled Rapid Discovery of Unique SARS‐CoV‐2 Mpro Inhibitors With Robust Potency and Drug‐like Profile
M Yang, MK Lee, S Gao, L Song, HY Jang… - Advanced …, 2024 - Wiley Online Library
The COVID‐19 pandemic has required an expeditious advancement of innovative antiviral
drugs. In this study, focused compound libraries are synthesized in 96‐well plates utilizing …
drugs. In this study, focused compound libraries are synthesized in 96‐well plates utilizing …
SARS-CoV-2 resistance to monoclonal antibodies and small-molecule drugs
Over four years have passed since the beginning of the COVID-19 pandemic. The scientific
response has been rapid and effective, with many therapeutic monoclonal antibodies and …
response has been rapid and effective, with many therapeutic monoclonal antibodies and …
Lessons learnt from the preclinical discovery and development of ensitrelvir as a COVID-19 therapeutic option
S Ferraro, I Convertino, E Cappello… - Expert Opinion on …, 2024 - Taylor & Francis
Introduction The COVID-19 pandemic stimulated the development of several therapeutic
tools with several degrees of success. Ensitrelvir, a protease inhibitor that blocks the …
tools with several degrees of success. Ensitrelvir, a protease inhibitor that blocks the …
Rational Design of Macrocyclic Noncovalent Inhibitors of SARS-CoV-2 Mpro from a DNA-Encoded Chemical Library Screening Hit That Demonstrate Potent Inhibition …
The recent global COVID-19 pandemic has highlighted treatments for coronavirus infection
as an unmet medical need. The main protease (Mpro) has been an important target for the …
as an unmet medical need. The main protease (Mpro) has been an important target for the …