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 …

SARS-CoV-2 resistance to monoclonal antibodies and small-molecule drugs

S Iketani, DD Ho - Cell Chemical Biology, 2024 - cell.com
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 …

Nirmatrelvir resistance—de novo E166V/L50V mutations in an immunocompromised patient treated with prolonged nirmatrelvir/ritonavir monotherapy leading to …

NS Zuckerman, E Bucris… - Clinical Infectious …, 2024 - academic.oup.com
Resistance of SARS-CoV-2 to antivirals was shown to develop in immunocompromised
individuals receiving remdesivir. We describe an immunocompromised patient who was …

An orally bioavailable SARS-CoV-2 main protease inhibitor exhibits improved affinity and reduced sensitivity to mutations

M Westberg, Y Su, X Zou, P Huang, A Rustagi… - Science translational …, 2024 - science.org
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 …

The importance of good practices and false hits for QSAR-driven virtual screening real application: a SARS-CoV-2 main protease (Mpro) case study

MSM Serafim, SQ Pantaleão, EB da Silva… - Frontiers in Drug …, 2023 - frontiersin.org
Computer-Aided Drug Design (CADD) approaches, such as those employing quantitative
structure-activity relationship (QSAR) methods, are known for their ability to uncover novel …

Resistance mechanisms of SARS-CoV-2 3CLpro to the non-covalent inhibitor WU-04

L Zhang, X Xie, H Luo, R Qian, Y Yang, H Yu, J Huang… - Cell Discovery, 2024 - nature.com
Drug resistance poses a significant challenge in the development of effective therapies
against SARS-CoV-2. Here, we identified two double mutations, M49K/M165V and …

Identification of a novel inhibitor of SARS-CoV-2 main protease: an in silico, biochemical, and cell-based approach

A Trivedi, V Kardam, KK Inampudi, S Vrati… - The FEBS …, 2023 - pubmed.ncbi.nlm.nih.gov
The recurrent nature of coronavirus outbreaks, severity of the COVID-19 pandemic, rapid
emergence of novel variants, and concerns over the effectiveness of existing vaccines …

Design of SARS-CoV-2 protease inhibitors with improved affinity and reduced sensitivity to mutations

M Westberg, Y Su, X Zou, P Huang, A Rustagi… - bioRxiv, 2023 - biorxiv.org
Inhibitors of the SARS-CoV-2 main protease (Mpro) such as nirmatrelvir (NTV) and
ensitrelvir (ETV) have proven effective in reducing the severity of COVID-19, but the …

Substitutions in SARS-CoV-2 Mpro Selected by Protease Inhibitor Boceprevir Confer Resistance to Nirmatrelvir

KA Gammeltoft, Y Zhou, LA Ryberg, LV Pham… - Viruses, 2023 - mdpi.com
Nirmatrelvir, which targets the SARS-CoV-2 main protease (Mpro), is the first-in-line drug for
prevention and treatment of severe COVID-19, and additional Mpro inhibitors are in …

[HTML][HTML] New anti-SARS-CoV-2 aminoadamantane compounds as antiviral candidates for the treatment of COVID-19

DP de Almeida Marques, LAF Andrade, EVS Reis… - Virus Research, 2024 - Elsevier
Here, the antiviral activity of aminoadamantane derivatives were evaluated against SARS-
CoV-2. The compounds exhibited low cytotoxicity to Vero, HEK293 and CALU-3 cells up to a …