Hotspot residues and resistance mutations in the nirmatrelvir-binding site of SARS-CoV-2 main protease: Design, identification, and correlation with globally …

AK Padhi, T Tripathi - Biochemical and Biophysical Research …, 2022 - Elsevier
Shortly after the onset of the COVID-19 pandemic, severe acute respiratory syndrome
coronavirus 2 (SARS-CoV-2) has acquired numerous variations in its intracellular proteins to …

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 SARS-CoV-2 main protease (Mpro) is the drug target of Pfizer's oral drug nirmatrelvir.
The emergence of SARS-CoV-2 variants with mutations in Mpro raised the alarm of potential …

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
SARS-CoV-2 continues to pose a threat to public health. Main protease (Mpro) is one of the
most lucrative drug targets for developing specific antivirals against SARS-CoV-2 infection …

[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 …

Genetic Surveillance of SARS-CoV-2 Mpro Reveals High Sequence and Structural Conservation Prior to the Introduction of Protease Inhibitor Paxlovid

JT Lee, Q Yang, A Gribenko, BS Perrin Jr, Y Zhu… - Mbio, 2022 - Am Soc Microbiol
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) continues to represent a
global health emergency as a highly transmissible, airborne virus. An important coronaviral …

[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
Coronavirus disease 2019 (COVID-19), caused by the severe acute respiratory syndrome 2
(SARS-CoV-2), has been one of the most devastating pandemics of recent times. The lack of …

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

S Ullrich, KB Ekanayake, G Otting, C Nitsche - Bioorganic & Medicinal …, 2022 - Elsevier
The COVID-19 pandemic continues to be a public health threat. Multiple mutations in the
spike protein of emerging variants of SARS-CoV-2 appear to impact on the effectiveness of …

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
Conspectus SARS-CoV-2 is the etiological pathogen of the COVID-19 pandemic, which led
to more than 6.5 million deaths since the beginning of the outbreak in December 2019. The …

[HTML][HTML] Defining the substrate envelope of SARS-CoV-2 main protease to predict and avoid drug resistance

AM Shaqra, SN Zvornicanin, QYJ Huang… - Nature …, 2022 - nature.com
Coronaviruses can evolve and spread rapidly to cause severe disease morbidity and
mortality, as exemplified by SARS-CoV-2 variants of the COVID-19 pandemic. Although …

Systematic analyses of the resistance potential of drugs targeting SARS-CoV-2 main protease

JM Flynn, QYJ Huang, SN Zvornicanin… - ACS infectious …, 2023 - ACS Publications
Drugs that target the main protease (Mpro) of SARS-CoV-2 are effective therapeutics that
have entered clinical use. Wide-scale use of these drugs will apply selection pressure for the …