Therapeutic strategies for COVID-19: progress and lessons learned

G Li, R Hilgenfeld, R Whitley, E De Clercq - Nature Reviews Drug …, 2023 - nature.com
Abstract The coronavirus disease 2019 (COVID-19) pandemic has stimulated tremendous
efforts to develop therapeutic strategies that target severe acute respiratory syndrome …

Therapeutics for COVID-19

SS Toussi, JL Hammond, BS Gerstenberger… - Nature …, 2023 - nature.com
Vaccines and monoclonal antibody treatments to prevent severe coronavirus disease 2019
(COVID-19) illness were available within a year of the pandemic being declared but there …

SARS-CoV-2 3CLpro mutations selected in a VSV-based system confer resistance to nirmatrelvir, ensitrelvir, and GC376

E Heilmann, F Costacurta, SA Moghadasi… - Science translational …, 2022 - science.org
Protease inhibitors are among the most powerful antiviral drugs. Nirmatrelvir is the first
protease inhibitor specifically developed against the SARS-CoV-2 protease 3CLpro that has …

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

Q Hu, Y Xiong, 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] Paxlovid (Nirmatrelvir/Ritonavir): A new approach to Covid-19 therapy?

SMR Hashemian, A Sheida, M Taghizadieh… - Biomedicine & …, 2023 - Elsevier
Despite the need for novel, effective therapeutics for the COVID-19 pandemic, no curative
regimen is yet available, therefore patients are forced to rely on supportive and nonspecific …

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 …

Structural basis of nirmatrelvir and ensitrelvir activity against naturally occurring polymorphisms of the SARS-CoV-2 main protease

GD Noske, E de Souza Silva, MO de Godoy… - Journal of Biological …, 2023 - ASBMB
SARS-CoV-2 is the causative agent of COVID-19. The main viral protease (M pro) is an
attractive target for antivirals. The clinically approved drug nirmatrelvir and the clinical …

Alkyne derivatives of SARS-CoV-2 main protease inhibitors including nirmatrelvir inhibit by reacting covalently with the Nucleophilic Cysteine

L Brewitz, L Dumjahn, Y Zhao, CD Owen… - Journal of Medicinal …, 2023 - ACS Publications
Nirmatrelvir (PF-07321332) is a nitrile-bearing small-molecule inhibitor that, in combination
with ritonavir, is used to treat infections by severe acute respiratory syndrome coronavirus-2 …

Molecular mechanism of ensitrelvir inhibiting SARS-CoV-2 main protease and its variants

M Lin, X Zeng, Y Duan, Z Yang, Y Ma, H Yang… - Communications …, 2023 - nature.com
SARS-CoV-2 poses an unprecedented threat to the world as the causative agent of the
COVID-19 pandemic. Among a handful of therapeutics developed for the prevention and …

Recent advances in SARS-CoV-2 main protease inhibitors: from nirmatrelvir to future perspectives

A Citarella, A Dimasi, D Moi, D Passarella, A Scala… - Biomolecules, 2023 - mdpi.com
The main protease (Mpro) plays a pivotal role in the replication of severe acute respiratory
syndrome coronavirus 2 (SARS-CoV-2) and is considered a highly conserved viral target …