Accelerating antiviral drug discovery: lessons from COVID-19

A Von Delft, MD Hall, AD Kwong, LA Purcell… - Nature Reviews Drug …, 2023 - nature.com
During the coronavirus disease 2019 (COVID-19) pandemic, a wave of rapid and
collaborative drug discovery efforts took place in academia and industry, culminating in …

Emerging and re-emerging warheads for targeted covalent inhibitors: an update

L Hillebrand, XJ Liang, RAM Serafim… - Journal of medicinal …, 2024 - ACS Publications
Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

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 …

An orally bioavailable SARS-CoV-2 main protease inhibitor exhibits improved affinity and reduced sensitivity to mutations

M Westberg, Y Su, X Zou, P Huang, A Rustagi… - Science translational …, 2024 - science.org
Inhibitors of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main
protease (Mpro) such as nirmatrelvir (NTV) and ensitrelvir (ETV) have proven effective in …

The SARS‐CoV‐2 main protease (Mpro): Structure, function, and emerging therapies for COVID‐19

Q Hu, Y **ong, GH Zhu, YN Zhang, YW Zhang… - MedComm, 2022 - Wiley Online Library
The main proteases (Mpro), also termed 3‐chymotrypsin‐like proteases (3CLpro), are a
class of highly conserved cysteine hydrolases in β‐coronaviruses. Increasing evidence has …

Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease

C Ma, MD Sacco, B Hurst, JA Townsend, Y Hu, T Szeto… - Cell research, 2020 - nature.com
A new coronavirus SARS-CoV-2, also called novel coronavirus 2019 (2019-nCoV), started
to circulate among humans around December 2019, and it is now widespread as a global …

Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease

L Fu, F Ye, Y Feng, F Yu, Q Wang, Y Wu, C Zhao… - Nature …, 2020 - nature.com
COVID-19 was declared a pandemic on March 11 by WHO, due to its great threat to global
public health. The coronavirus main protease (Mpro, also called 3CLpro) is essential for …

Targeting SARS-CoV-2 main protease for treatment of COVID-19: Covalent inhibitors structure–activity relationship insights and evolution perspectives

G La Monica, A Bono, A Lauria… - Journal of medicinal …, 2022 - ACS Publications
The viral main protease is one of the most attractive targets among all key enzymes involved
in the SARS-CoV-2 life cycle. Covalent inhibition of the cysteine145 of SARS-CoV-2 MPRO …

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 …

Feline coronavirus drug inhibits the main protease of SARS-CoV-2 and blocks virus replication

W Vuong, MB Khan, C Fischer, E Arutyunova… - Nature …, 2020 - nature.com
The main protease, Mpro (or 3CLpro) in SARS-CoV-2 is a viable drug target because of its
essential role in the cleavage of the virus polypeptide. Feline infectious peritonitis, a fatal …