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Targeting SARS-CoV-2 main protease for treatment of COVID-19: Covalent inhibitors structure–activity relationship insights and evolution perspectives
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 …
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
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 …
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
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 …
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
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 …
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
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 …
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
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 …
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
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 …
syndrome coronavirus 2 (SARS-CoV-2) and is considered a highly conserved viral target …
Targeting SARS-CoV-2 proteases for COVID-19 antiviral development
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 …
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 …
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 …
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
Small molecule drugs that covalently bind irreversibly to their target proteins have several
advantages over conventional reversible inhibitors. They include increased duration of …
advantages over conventional reversible inhibitors. They include increased duration of …