The SARS-CoV-2 main protease as drug target

S Ullrich, C Nitsche - Bioorganic & medicinal chemistry letters, 2020 - Elsevier
The unprecedented pandemic of the severe acute respiratory syndrome coronavirus 2
(SARS-CoV-2) is threatening global health. The virus emerged in late 2019 and can cause a …

Structure and function of SARS-CoV and SARS-CoV-2 main proteases and their inhibition: A comprehensive review

X Li, Y Song - European Journal of Medicinal Chemistry, 2023 - Elsevier
Severe acute respiratory syndrome-associated coronavirus (SARS-CoV) identified in 2003
infected∼ 8000 people in 26 countries with 800 deaths, which was soon contained and …

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 …

Structure and inhibition of the SARS-CoV-2 main protease reveal strategy for developing dual inhibitors against Mpro and cathepsin L

MD Sacco, C Ma, P Lagarias, A Gao, JA Townsend… - Science …, 2020 - science.org
The main protease (Mpro) of SARS-CoV-2 is a key antiviral drug target. While most Mpro
inhibitors have a γ-lactam glutamine surrogate at the P1 position, we recently found that …

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 …

α-Ketoamides as broad-spectrum inhibitors of coronavirus and enterovirus replication: structure-based design, synthesis, and activity assessment

L Zhang, D Lin, Y Kusov, Y Nian, Q Ma… - Journal of medicinal …, 2020 - ACS Publications
The main protease of coronaviruses and the 3C protease of enteroviruses share a similar
active-site architecture and a unique requirement for glutamine in the P1 position of the …

SARS-CoV-2 Mpro inhibitors and activity-based probes for patient-sample imaging

W Rut, K Groborz, L Zhang, X Sun… - Nature chemical …, 2021 - nature.com
In December 2019, the first cases of infection with a novel coronavirus, SARS-CoV-2, were
diagnosed. Currently, there is no effective antiviral treatment for COVID-19. To address this …

Covalent narlaprevir-and boceprevir-derived hybrid inhibitors of SARS-CoV-2 main protease

DW Kneller, H Li, G Phillips, KL Weiss, Q Zhang… - Nature …, 2022 - nature.com
Emerging SARS-CoV-2 variants continue to threaten the effectiveness of COVID-19
vaccines, and small-molecule antivirals can provide an important therapeutic treatment …

Nelfinavir was predicted to be a potential inhibitor of 2019-nCov main protease by an integrative approach combining homology modelling, molecular docking and …

Z Xu, C Peng, Y Shi, Z Zhu, K Mu, X Wang, W Zhu - BioRxiv, 2020 - biorxiv.org
nCov has caused more than 80 deaths as of 27 January 2020 in China, and infection cases
have been reported in more than 10 countries. However, there is no approved drug to treat …

Drug development and medicinal chemistry efforts toward SARS‐coronavirus and Covid‐19 therapeutics

AK Ghosh, M Brindisi, D Shahabi… - …, 2020 - Wiley Online Library
The COVID‐19 pandemic caused by SARS‐CoV‐2 infection is spreading at an alarming
rate and has created an unprecedented health emergency around the globe. There is no …