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Accelerating antiviral drug discovery: lessons from COVID-19
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 …
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 …
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
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 …
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 …
coronavirus disease 2019 (COVID-19). To facilitate resistance monitoring, we studied …
A living WHO guideline on drugs for covid-19
Updates This is the fourteenth version (thirteenth update) of the living guideline, replacing
earlier versions (available as data supplements). New recommendations will be published …
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
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 …
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
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 …
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 …
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
The coronavirus spike glycoprotein attaches to host receptors and mediates viral fusion.
Using a broad screening approach, we isolated seven monoclonal antibodies (mAbs) that …
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 …
Nsp5), is clinically useful against SARS-CoV-2 including its omicron variants. Since most …