An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19

DR Owen, CMN Allerton, AS Anderson… - Science, 2021 - science.org
The worldwide outbreak of COVID-19 caused by severe acute respiratory syndrome
coronavirus 2 (SARS-CoV-2) has become a global pandemic. Alongside vaccines, antiviral …

X-ray screening identifies active site and allosteric inhibitors of SARS-CoV-2 main protease

S Günther, PYA Reinke, Y Fernández-García, J Lieske… - Science, 2021 - science.org
The coronavirus disease (COVID-19) caused by SARS-CoV-2 is creating tremendous
human suffering. To date, no effective drug is available to directly treat the disease. In a …

SARS-CoV-2 Mpro inhibitors with antiviral activity in a transgenic mouse model

J Qiao, YS Li, R Zeng, FL Liu, RH Luo, C Huang… - Science, 2021 - science.org
The COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2
(SARS-CoV-2) continually poses serious threats to global public health. The main protease …

Identification of SARS-CoV-2 Mpro inhibitors containing P1' 4-fluorobenzothiazole moiety highly active against SARS-CoV-2

N Higashi-Kuwata, K Tsuji, H Hayashi, H Bulut… - Nature …, 2023 - nature.com
COVID-19 caused by SARS-CoV-2 has continually been serious threat to public health
worldwide. While a few anti-SARS-CoV-2 therapeutics are currently available, their antiviral …

Evaluation of SARS-CoV-2 main protease inhibitors using a novel cell-based assay

W Cao, CCD Cho, ZZ Geng, N Shaabani… - ACS central …, 2022 - ACS Publications
As an essential enzyme of SARS-CoV-2, main protease (MPro) triggers acute toxicity to its
human cell host, an effect that can be alleviated by an MPro inhibitor. Using this toxicity …

S-217622, a SARS-CoV-2 main protease inhibitor, decreases viral load and ameliorates COVID-19 severity in hamsters

M Sasaki, K Tabata, M Kishimoto, Y Itakura… - Science translational …, 2022 - science.org
In parallel with vaccination, oral antiviral agents are highly anticipated to act as
countermeasures for the treatment of the coronavirus disease 2019 (COVID-19) pandemic …

Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors

L Zhang, D Lin, X Sun, U Curth, C Drosten… - Science, 2020 - science.org
The coronavirus disease 2019 (COVID-19) pandemic caused by severe acute respiratory
syndrome–coronavirus 2 (SARS-CoV-2) is a global health emergency. An attractive drug …

Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19

B Boras, RM Jones, BJ Anson, D Arenson… - Nature …, 2021 - nature.com
COVID-19 caused by the SARS-CoV-2 virus has become a global pandemic. 3CL protease
is a virally encoded protein that is essential across a broad spectrum of coronaviruses with …

Discovery and mechanism of SARS-CoV-2 main protease inhibitors

S Huff, IR Kummetha, SK Tiwari… - Journal of medicinal …, 2021 - ACS Publications
The emergence of a new coronavirus, severe acute respiratory syndrome coronavirus 2
(SARS-CoV-2), presents an urgent public health crisis. Without available targeted therapies …

Perspectives on SARS-CoV-2 main protease inhibitors

K Gao, R Wang, J Chen, JJ Tepe… - Journal of medicinal …, 2021 - ACS Publications
The main protease (Mpro) plays a crucial role in severe acute respiratory syndrome
coronavirus 2 (SARS-CoV-2) replication and is highly conserved, rendering it one of the …