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 …

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 …

[HTML][HTML] Remdesivir, Molnupiravir and Nirmatrelvir remain active against SARS-CoV-2 Omicron and other variants of concern

L Vangeel, W Chiu, S De Jonghe, P Maes, B Slechten… - Antiviral research, 2022 - Elsevier
We assessed the in vitro antiviral activity of remdesivir and its parent nucleoside GS-441524,
molnupiravir and its parent nucleoside EIDD-1931 and the viral protease inhibitor …

Nirmatrelvir-resistant SARS-CoV-2 variants with high fitness in an infectious cell culture system

Y Zhou, KA Gammeltoft, LA Ryberg, LV Pham… - Science …, 2022 - science.org
The oral protease inhibitor nirmatrelvir is of key importance for prevention of severe
coronavirus disease 2019 (COVID-19). To facilitate resistance monitoring, we studied …

A living WHO guideline on drugs for covid-19

A Agarwal, BJ Hunt, M Stegemann, B Rochwerg… - bmj, 2020 - bmj.com
Updates This is the fourteenth version (thirteenth update) of the living guideline, replacing
earlier versions (available as data supplements). New recommendations will be published …

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 …

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 …

The Substitutions L50F, E166A, and L167F in SARS-CoV-2 3CLpro Are Selected by a Protease Inhibitor In Vitro and Confer Resistance To Nirmatrelvir

D Jochmans, C Liu, K Donckers, A Stoycheva… - MBio, 2023 - journals.asm.org
The SARS-CoV-2 main protease (3CLpro) has an indispensable role in the viral life cycle
and is a therapeutic target for the treatment of COVID-19. The potential of 3CLpro-inhibitors …

ACE2-binding exposes the SARS-CoV-2 fusion peptide to broadly neutralizing coronavirus antibodies

JS Low, J Jerak, MA Tortorici, M McCallum, D Pinto… - Science, 2022 - science.org
The coronavirus spike glycoprotein attaches to host receptors and mediates viral fusion.
Using a broad screening approach, we isolated seven monoclonal antibodies (mAbs) that …

In vitro and in vivo characterization of SARS-CoV-2 resistance to ensitrelvir

M Kiso, S Yamayoshi, S Iida, Y Furusawa… - Nature …, 2023 - nature.com
Ensitrelvir, an oral antiviral agent that targets a SARS-CoV-2 main protease (3CLpro or
Nsp5), is clinically useful against SARS-CoV-2 including its omicron variants. Since most …