[PDF][PDF] Preparing for the next viral threat with broad-spectrum antivirals
There is a large global unmet need for the development of countermeasures to combat
hundreds of viruses known to cause human disease and for the establishment of a …
hundreds of viruses known to cause human disease and for the establishment of a …
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 …
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 …
Transmissible SARS-CoV-2 variants with resistance to clinical protease inhibitors
Vaccines and drugs have helped reduce disease severity and blunt the spread of severe
acute respiratory syndrome coronavirus 2 (SARS-CoV-2). However, ongoing virus …
acute respiratory syndrome coronavirus 2 (SARS-CoV-2). However, ongoing virus …
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 …
[HTML][HTML] Pharmacological disruption of mSWI/SNF complex activity restricts SARS-CoV-2 infection
Identification of host determinants of coronavirus infection informs mechanisms of viral
pathogenesis and can provide new drug targets. Here we demonstrate that mammalian …
pathogenesis and can provide new drug targets. Here we demonstrate that mammalian …
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 - Am Soc Microbiol
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 …
[HTML][HTML] 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 …
[HTML][HTML] 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 …
[HTML][HTML] A new generation Mpro inhibitor with potent activity against SARS-CoV-2 Omicron variants
C Huang, H Shuai, J Qiao, Y Hou, R Zeng… - … and Targeted Therapy, 2023 - nature.com
Abstract Emerging SARS-CoV-2 variants, particularly the Omicron variant and its
sublineages, continually threaten the global public health. Small molecule antivirals are an …
sublineages, continually threaten the global public health. Small molecule antivirals are an …