Transmissible SARS-CoV-2 variants with resistance to clinical protease inhibitors

SA Moghadasi, E Heilmann, AM Khalil, C Nnabuife… - Science …, 2023 - science.org
Vaccines and drugs have helped reduce disease severity and blunt the spread of severe
acute respiratory syndrome coronavirus 2 (SARS-CoV-2). However, ongoing virus …

SARS-CoV-2 3CLpro mutations selected in a VSV-based system confer resistance to nirmatrelvir, ensitrelvir, and GC376

E Heilmann, F Costacurta, SA Moghadasi… - Science translational …, 2022 - science.org
Protease inhibitors are among the most powerful antiviral drugs. Nirmatrelvir is the first
protease inhibitor specifically developed against the SARS-CoV-2 protease 3CLpro that has …

Viral target and metabolism‐based rationale for combined use of recently authorized small molecule COVID‐19 medicines: Molnupiravir, nirmatrelvir, and remdesivir

D Yan, B Yan - Fundamental & Clinical Pharmacology, 2023 - Wiley Online Library
The COVID‐19 pandemic remains a major health concern worldwide, and SARS‐CoV‐2 is
continuously evolving. There is an urgent need to identify new antiviral drugs and develop …

Ebselen derivatives inhibit SARS-CoV-2 replication by inhibition of its essential proteins: PLpro and Mpro proteases, and nsp14 guanine N7-methyltransferase

M Zmudzinski, W Rut, K Olech, J Granda, M Giurg… - Scientific reports, 2023 - nature.com
Proteases encoded by SARS-CoV-2 constitute a promising target for new therapies against
COVID-19. SARS-CoV-2 main protease (Mpro, 3CLpro) and papain-like protease (PLpro) …

Lessons from SARS‑CoV‑2 and its variants

Z Qin, Y Sun, J Zhang, L Zhou… - Molecular …, 2022 - spandidos-publications.com
COVID‑19 has swept through mainland China by human‑to‑human transmission. The rapid
spread of SARS‑CoV‑2 and its variants, including the currently prevalent Omicron strain …

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 …

New insights in the mechanism of the SARS-CoV-2 Mpro inhibition by benzisoselenazolones and diselenides

L Sancineto, F Mangiavacchi, A Dabrowska… - Scientific Reports, 2024 - nature.com
Although global vaccination campaigns alleviated the SARS-CoV-2 pandemic in terms of
morbidity and mortality, the ability of the virus to originate mutants may reduce the efficacy of …

Study of key residues in MERS-CoV and SARS-CoV-2 main proteases for resistance against clinically applied inhibitors nirmatrelvir and ensitrelvir

L Krismer, H Schöppe, S Rauch, D Bante, B Sprenger… - npj Viruses, 2024 - nature.com
Abstract The Middle East Respiratory Syndrome Coronavirus (MERS-CoV) is an epidemic,
zoonotically emerging pathogen initially reported in Saudi Arabia in 2012. MERS-CoV has …

Proteolytic cleavage and inactivation of the TRMT1 tRNA modification enzyme by SARS-CoV-2 main protease

K Zhang, P Eldin, JH Ciesla, L Briant, JM Lentini… - Elife, 2024 - elifesciences.org
Abstract Nonstructural protein 5 (Nsp5) is the main protease of SARS-CoV-2 that cleaves
viral polyproteins into individual polypeptides necessary for viral replication. Here, we show …

A comprehensive study of SARS-CoV-2 main protease (Mpro) inhibitor-resistant mutants selected in a VSV-based system

F Costacurta, A Dodaro, D Bante, H Schöppe… - PLoS …, 2024 - journals.plos.org
Nirmatrelvir was the first protease inhibitor specifically developed against the SARS-CoV-2
main protease (3CLpro/Mpro) and licensed for clinical use. As SARS-CoV-2 continues to …