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 research progress of SARS-CoV-2 main protease inhibitors from 2020 to 2022

X Pang, W Xu, Y Liu, H Li, L Chen - European journal of medicinal …, 2023‏ - Elsevier
The novel coronavirus disease 2019 (COVID-19) caused by severe acute respiratory
syndrome coronavirus 2 (SARS-CoV-2) has spread worldwide. The main protease (M pro) of …

Evolutionary and structural insights about potential SARS-CoV-2 evasion of nirmatrelvir

KS Yang, SZ Leeuwon, S Xu… - Journal of medicinal …, 2022‏ - ACS Publications
The US FDA approval of PAXLOVID, a combination therapy of nirmatrelvir and ritonavir has
significantly boosted our morale in fighting the COVID-19 pandemic. Nirmatrelvir is an …

Development of optimized drug-like small molecule inhibitors of the SARS-CoV-2 3CL protease for treatment of COVID-19

H Liu, S Iketani, A Zask, N Khanizeman… - Nature …, 2022‏ - nature.com
Abstract The SARS-CoV-2 3CL protease is a critical drug target for small molecule COVID-
19 therapy, given its likely druggability and essentiality in the viral maturation and replication …

SARS-CoV-2 Mpro Protease Variants of Concern Display Altered Viral Substrate and Cell Host Target Galectin-8 Processing but Retain Sensitivity toward Antivirals

SA Chen, E Arutyunova, J Lu, MB Khan… - ACS Central …, 2023‏ - ACS Publications
The main protease of SARS-CoV-2 (Mpro) is the most promising drug target against
coronaviruses due to its essential role in virus replication. With newly emerging variants …

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 …

Targeting SARS-CoV-2 proteases for COVID-19 antiviral development

Z Lv, KE Cano, L Jia, M Drag, TT Huang… - Frontiers in …, 2022‏ - frontiersin.org
The emergence of severe acute respiratory syndrome (SARS-CoV-2) in 2019 marked the
third occurrence of a highly pathogenic coronavirus in the human population since 2003. As …

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 …

An update on the discovery and development of reversible covalent inhibitors

Faridoon, R Ng, G Zhang, JJ Li - Medicinal Chemistry Research, 2023‏ - Springer
Small molecule drugs that covalently bind irreversibly to their target proteins have several
advantages over conventional reversible inhibitors. They include increased duration of …