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 …
worldwide as a consequence of being the most disastrous infectious disease in the past …
Proline Analogues
V Kubyshkin, M Rubini - Chemical Reviews, 2024 - ACS Publications
Within the canonical repertoire of the amino acid involved in protein biogenesis, proline
plays a unique role as an amino acid presenting a modified backbone rather than a side …
plays a unique role as an amino acid presenting a modified backbone rather than a side …
Naturally occurring mutations of SARS-CoV-2 main protease confer drug resistance to nirmatrelvir
The SARS-CoV-2 main protease (Mpro) is the drug target of Pfizer's oral drug nirmatrelvir.
The emergence of SARS-CoV-2 variants with mutations in Mpro raised the alarm of potential …
The emergence of SARS-CoV-2 variants with mutations in Mpro raised the alarm of potential …
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 …
Global prevalence of SARS-CoV-2 3CL protease mutations associated with nirmatrelvir or ensitrelvir resistance
JD Ip, AWH Chu, WM Chan, RCY Leung… - …, 2023 - thelancet.com
Summary Background Nirmatrelvir-ritonavir (Paxlovid) and ensitrelvir are 3-chymotrypsin-
like cysteine protease (3CL pro) inhibitors which have been approved for the treatment of …
like cysteine protease (3CL pro) inhibitors which have been approved for the treatment of …
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 …
COVID-19 pandemic. Among a handful of therapeutics developed for the prevention and …
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 …
Emerging SARS-CoV-2 resistance after antiviral treatment
TJ Tamura, MC Choudhary, R Deo, F Yousuf… - JAMA Network …, 2024 - jamanetwork.com
Importance Previous studies have identified mutations in SARS-CoV-2 strains that confer
resistance to nirmatrelvir, yet how often this resistance arises and its association with …
resistance to nirmatrelvir, yet how often this resistance arises and its association with …
Proof-of-concept studies with a computationally designed Mpro inhibitor as a synergistic combination regimen alternative to Paxlovid
As the SARS-CoV-2 virus continues to spread and mutate, it remains important to focus not
only on preventing spread through vaccination but also on treating infection with direct …
only on preventing spread through vaccination but also on treating infection with direct …
Development of de-novo coronavirus 3-chymotrypsin-like protease (3CLpro) inhibitors since COVID-19 outbreak: A strategy to tackle challenges of persistent virus …
L Tian, T Qiang, X Yang, Y Gao, X Zhai, K Kang… - European Journal of …, 2024 - Elsevier
Although no longer a public health emergency of international concern, COVID-19 remains
a persistent and critical health concern. The development of effective antiviral drugs could …
a persistent and critical health concern. The development of effective antiviral drugs could …