[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
Nirmatrelvir, an oral antiviral targeting the 3CL protease of SARS-CoV-2, has been
demonstrated to be clinically useful against COVID-19 (refs.,). However, because SARS …

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 …

Computational protein design for COVID-19 research and emerging therapeutics

P Kalita, T Tripathi, AK Padhi - ACS Central Science, 2023 - ACS Publications
As the world struggles with the ongoing COVID-19 pandemic, unprecedented obstacles
have continuously been traversed as new SARS-CoV-2 variants continually emerge …

[HTML][HTML] Structural basis of nirmatrelvir and ensitrelvir activity against naturally occurring polymorphisms of the SARS-CoV-2 main protease

GD Noske, E de Souza Silva, MO de Godoy… - Journal of Biological …, 2023 - ASBMB
SARS-CoV-2 is the causative agent of COVID-19. The main viral protease (M pro) is an
attractive target for antivirals. The clinically approved drug nirmatrelvir and the clinical …

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 …

Alkyne as a Latent Warhead to Covalently Target SARS-CoV-2 Main Protease

C Ngo, W Fried, S Aliyari, J Feng, C Qin… - Journal of Medicinal …, 2023 - ACS Publications
There is an urgent need for improved therapy to better control the ongoing COVID-19
pandemic. The main protease Mpro plays a pivotal role in SARS-CoV-2 replications, thereby …

[HTML][HTML] Resistance to nirmatrelvir due to mutations in the Mpro in the subvariants of SARS-CoV-2 Omicron: Another concern?

S Chatterjee, M Bhattacharya, K Dhama, SS Lee… - … Therapy-Nucleic Acids, 2023 - cell.com
The world has faced 3 years of the COVID-19 pandemic with billions of infections, millions of
deaths, and a massive economic crisis. Since the pandemic began, scientists have started to …

[HTML][HTML] A yeast-based system to study SARS-CoV-2 Mpro structure and to identify nirmatrelvir resistant mutations

J Ou, EM Lewandowski, Y Hu, AA Lipinski… - PLoS …, 2023 - journals.plos.org
The SARS-CoV-2 main protease (Mpro) is a major therapeutic target. The Mpro inhibitor,
nirmatrelvir, is the antiviral component of Paxlovid, an orally available treatment for COVID …

[HTML][HTML] The impact of SARS-CoV-2 3CL protease mutations on nirmatrelvir inhibitory efficiency. Computational insights into potential resistance mechanisms

CA Ramos-Guzmán, M Andjelkovic, K Zinovjev… - Chemical …, 2023 - pubs.rsc.org
The use of antiviral drugs can promote the appearance of mutations in the target protein that
increase the resistance of the virus to the treatment. This is also the case of nirmatrelvir, a …

[HTML][HTML] Crystal structures of main protease (Mpro) mutants of SARS-CoV-2 variants bound to PF-07304814

H Jiang, X Zou, P Zeng, X Zeng, X Zhou, J Wang… - Molecular …, 2023 - Springer
There is an urgent need to develop effective antiviral drugs to prevent the viral infection
caused by constantly circulating SARS-CoV-2 as well as its variants. The main protease …