Design of a SARS-CoV-2 papain-like protease inhibitor with antiviral efficacy in a mouse model

B Tan, X Zhang, A Ansari, P Jadhav, H Tan, K Li… - Science, 2024 - science.org
The emergence of SARS-CoV-2 variants and drug-resistant mutants calls for additional oral
antivirals. The SARS-CoV-2 papain-like protease (PLpro) is a promising but challenging …

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 …

Discovery of SARS-CoV-2 papain-like protease inhibitors through a combination of high-throughput screening and a FlipGFP-based reporter assay

C Ma, MD Sacco, Z Xia, G Lambrinidis… - ACS central …, 2021 - ACS Publications
The papain-like protease (PLpro) of SARS-CoV-2 is a validated antiviral drug target.
Through a fluorescence resonance energy transfer-based high-throughput screening and …

<? covid19?> High-Throughput Screening for Drugs That Inhibit Papain-Like Protease in SARS-CoV-2

E Smith, ME Davis-Gardner… - … the Science of Drug …, 2020 - journals.sagepub.com
The emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in late
2019 has triggered an ongoing global pandemic whereby infection may result in a lethal …

Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2

H Shan, J Liu, J Shen, J Dai, G Xu, K Lu, C Han… - Cell chemical …, 2021 - cell.com
The COVID-19 pandemic has been disastrous to society and effective drugs are urgently
needed. The papain-like protease domain (PLpro) of SARS-CoV-2 (SCoV2) is …

Structure of papain-like protease from SARS-CoV-2 and its complexes with non-covalent inhibitors

J Osipiuk, SA Azizi, S Dvorkin, M Endres… - Nature …, 2021 - nature.com
The pandemic caused by Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-
2) continues to expand. Papain-like protease (PLpro) is one of two SARS-CoV-2 proteases …

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 …

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 …

NMR Characterization of the Papain-like Protease from SARS-CoV-2 Identifies the Conformational Heterogeneity in Its Inhibitor-Binding Site

Y Shiraishi, I Shimada - Journal of the American Chemical Society, 2023 - ACS Publications
Papain-like protease (PLpro) from severe acute respiratory syndrome Coronavirus 2 (SARS-
CoV-2) is a prime target for the development of antivirals for Coronavirus disease 2019 …