Bench-to-bedside: Innovation of small molecule anti-SARS-CoV-2 drugs in China

L Yang, Z Wang - European Journal of Medicinal Chemistry, 2023 - Elsevier
The ongoing COVID-19 pandemic has resulted in millions of deaths globally, highlighting
the need to develop potent prophylactic and therapeutic strategies against SARS-CoV-2 …

SARS-CoV-2 main protease drug design, assay development, and drug resistance studies

B Tan, R Joyce, H Tan, Y Hu… - Accounts of chemical …, 2022 - ACS Publications
Conspectus SARS-CoV-2 is the etiological pathogen of the COVID-19 pandemic, which led
to more than 6.5 million deaths since the beginning of the outbreak in December 2019. The …

Transmissible SARS-CoV-2 variants with resistance to clinical protease inhibitors

SA Moghadasi, E Heilmann, AM Khalil, C Nnabuife… - Science …, 2023 - science.org
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 …

SARS-CoV-2 3CLpro mutations selected in a VSV-based system confer resistance to nirmatrelvir, ensitrelvir, and GC376

E Heilmann, F Costacurta, SA Moghadasi… - Science translational …, 2022 - science.org
Protease inhibitors are among the most powerful antiviral drugs. Nirmatrelvir is the first
protease inhibitor specifically developed against the SARS-CoV-2 protease 3CLpro that has …

[HTML][HTML] Pharmacological disruption of mSWI/SNF complex activity restricts SARS-CoV-2 infection

J Wei, A Patil, CK Collings, MM Alfajaro, Y Liang… - Nature Genetics, 2023 - nature.com
Identification of host determinants of coronavirus infection informs mechanisms of viral
pathogenesis and can provide new drug targets. Here we demonstrate that mammalian …

[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 …

[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 …

A conserved oligomerization domain in the disordered linker of coronavirus nucleocapsid proteins

H Zhao, D Wu, SA Hassan, A Nguyen, J Chen… - Science …, 2023 - science.org
The nucleocapsid (N-) protein of severe acute respiratory syndrome coronavirus 2 (SARS-
CoV-2) has a key role in viral assembly and scaffolding of the viral RNA. It promotes liquid …

[HTML][HTML] Structural basis of nirmatrelvir and ensitrelvir activity against naturally occurring polymorphisms of the SARS-CoV-2 main protease

GD Noske, E de Souza Silva, MO de Godoy… - Journal of Biological …, 2023 - ASBMB
SARS-CoV-2 is the causative agent of COVID-19. The main viral protease (M pro) is an
attractive target for antivirals. The clinically approved drug nirmatrelvir and the clinical …

[HTML][HTML] Viral burden rebound in hospitalised patients with COVID-19 receiving oral antivirals in Hong Kong: a population-wide retrospective cohort study

CKH Wong, KTK Lau, ICH Au, EHY Lau… - The Lancet Infectious …, 2023 - thelancet.com
Background Viral rebound after nirmatrelvir–ritonavir treatment has implications for the
clinical management and isolation of patients with COVID-19. We evaluated an unselected …