Nirmatrelvir, Molnupiravir, and Remdesivir maintain potent in vitro activity against the SARS-CoV-2 Omicron variant

R Rosales, BL McGovern, ML Rodriguez, DK Rai… - BioRxiv, 2022 - biorxiv.org
Variants of SARS-CoV-2 have become a major public health concern due to increased
transmissibility, and escape from natural immunity, vaccine protection, and monoclonal …

[HTML][HTML] Structure-based development and preclinical evaluation of the SARS-CoV-2 3C-like protease inhibitor simnotrelvir

X Jiang, H Su, W Shang, F Zhou, Y Zhang… - Nature …, 2023 - nature.com
The persistent pandemic of coronavirus disease 2019 (COVID-19) caused by severe acute
respiratory syndrome coronavirus 2 (SARS-CoV-2) and its variants accentuates the great …

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 …

[PDF][PDF] Functional map of SARS-CoV-2 3CL protease reveals tolerant and immutable sites

S Iketani, SJ Hong, J Sheng, F Bahari, B Culbertson… - Cell Host & Microbe, 2022 - cell.com
Summary The SARS-CoV-2 3CL protease (3CL pro) is an attractive therapeutic target, as it
is essential to the virus and highly conserved among coronaviruses. However, our current …

Alkyne derivatives of SARS-CoV-2 main protease inhibitors including nirmatrelvir inhibit by reacting covalently with the Nucleophilic Cysteine

L Brewitz, L Dumjahn, Y Zhao, CD Owen… - Journal of Medicinal …, 2023 - ACS Publications
Nirmatrelvir (PF-07321332) is a nitrile-bearing small-molecule inhibitor that, in combination
with ritonavir, is used to treat infections by severe acute respiratory syndrome coronavirus-2 …

[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 …

Disposition of nirmatrelvir, an orally bioavailable inhibitor of SARS-CoV-2 3C-like protease, across animals and humans

H Eng, AL Dantonio, EP Kadar, RS Obach, L Di… - Drug Metabolism and …, 2022 - ASPET
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3C-like protease
inhibitor PF-07321332 (nirmatrelvir), in combination with ritonavir (Paxlovid), was recently …

[HTML][HTML] The history, mechanism, and perspectives of nirmatrelvir (PF-07321332): an orally bioavailable main protease inhibitor used in combination with ritonavir to …

RP Joyce, VW Hu, J Wang - Medicinal Chemistry Research, 2022 - Springer
The rapid development of effective vaccines to combat the SARS-CoV-2 virus has been an
effective counter measure to decrease hospitalization and the mortality rate in many …

Efficacy comparison of 3CL protease inhibitors ensitrelvir and nirmatrelvir against SARS-CoV-2 in vitro and in vivo

T Kuroda, H Nobori, K Fukao, K Baba… - Journal of …, 2023 - academic.oup.com
Objectives Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become
established in the human population, making the need to develop safe and effective …

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 …