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 …

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 …

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 …

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 …

The history, mechanism, and perspectives of nirmatrelvir (PF-07321332): an orally bioavailable main protease inhibitor used in combination with ritonavir to reduce …

RP Joyce, VW Hu, J Wang - Medicinal Chemistry Research, 2022 - Springer
The rapid development of effective vaccines to combat the SARS-CoV-2 virus has been an
effective counter measure to decrease hospitalization and the mortality rate in many …

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 …

Discovery and crystallographic studies of trisubstituted piperazine derivatives as non-covalent SARS-CoV-2 main protease inhibitors with high target specificity and …

S Gao, K Sylvester, L Song, T Claff, L Jing… - Journal of Medicinal …, 2022 - ACS Publications
The continuous spread of SARS-CoV-2 calls for more direct-acting antiviral agents to
combat the highly infectious variants. The main protease (Mpro) is an promising target for …

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 …

Small-molecule thioesters as SARS-CoV-2 main protease inhibitors: enzyme inhibition, structure–activity relationships, antiviral activity, and X-ray structure …

T Pillaiyar, P Flury, N Krüger, H Su… - Journal of Medicinal …, 2022 - ACS Publications
The main protease (Mpro, 3CLpro) of SARS-CoV-2 is an attractive target in coronaviruses
because of its crucial involvement in viral replication and transcription. Here, we report on …

Structural biology of SARS-CoV-2 Mpro and drug discovery

Y Duan, H Wang, Z Yuan, H Yang - Current Opinion in Structural Biology, 2023 - Elsevier
Since its outbreak in late 2019, the COVID-19 pandemic has drawn enormous attention
worldwide as a consequence of being the most disastrous infectious disease in the past …