Discovery of SARS-CoV-2 papain-like protease (PLpro) inhibitors with efficacy in a murine infection model

MR Garnsey, MC Robinson, LT Nguyen, R Cardin… - Science …, 2024 - science.org
Vaccines and first-generation antiviral therapeutics have provided important protection
against COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV …

Structural review of SARS-CoV-2 antiviral targets

W Cui, Y Duan, Y Gao, W Wang, H Yang - Structure, 2024 - cell.com
Summary The coronavirus disease 2019 (COVID-19), the disease caused by the severe
acute respiratory syndrome coronavirus 2 (SARS-CoV-2), represents the most disastrous …

Fixing the Achilles Heel of Pfizer's Paxlovid for COVID-19 Treatment

L Brewitz, CJ Schofield - Journal of Medicinal Chemistry, 2024 - ACS Publications
Nirmatrelvir (PF-07321332), a first-in-class inhibitor of the severe acute respiratory
syndrome coronavirus-2 (SARS-CoV-2) main protease (Mpro), was developed by Pfizer …

Discovery of orally bioavailable SARS-CoV-2 papain-like protease inhibitor as a potential treatment for COVID-19

Y Lu, Q Yang, T Ran, G Zhang, W Li, P Zhou… - Nature …, 2024 - nature.com
The RNA-dependent RNA polymerase (RdRp), 3C-like protease (3CLpro), and papain-like
protease (PLpro) are pivotal components in the viral life cycle of SARS-CoV-2, presenting as …

[HTML][HTML] Design of inhibitors of SARS-CoV-2 papain-like protease deriving from GRL0617: Structure–activity relationships

L Kerti, V Frecer - Bioorganic & Medicinal Chemistry, 2024 - Elsevier
The unique and complex structure of papain-like protease (PL pro) of the SARS-CoV-2 virus
represents a difficult challenge for antiviral development, yet it offers a compelling validated …

Preclinical and clinical investigations of potential drugs and vaccines for COVID-19 therapy: a comprehensive review with recent update

ME Mia, M Howlader, F Akter… - Clinical Pathology, 2024 - journals.sagepub.com
The COVID-19 pandemic-led worldwide healthcare crisis necessitates prompt societal,
ecological, and medical efforts to stop or reduce the rising number of fatalities. Numerous …

Covalent DNA-Encoded Library Workflow Drives Discovery of SARS-CoV-2 Nonstructural Protein Inhibitors

X Wang, L Xiong, Y Zhu, S Liu, W Zhao… - Journal of the …, 2024 - ACS Publications
The COVID-19 pandemic, exacerbated by persistent viral mutations, underscored the urgent
need for diverse inhibitors targeting multiple viral proteins. In this study, we utilized covalent …

Arylamines QSAR-Based Design and Molecular Dynamics of New Phenylthiophene and Benzimidazole Derivatives with Affinity for the C111, Y268, and H73 Sites of …

G Sabadini, M Mellado, C Morales, J Mella - Pharmaceuticals, 2024 - mdpi.com
A non-structural SARS-CoV-2 protein, PLpro, is involved in post-translational modifications
in cells, allowing the evasion of antiviral immune response mechanisms. In this study …

Structure-Based Design of Covalent SARS-CoV-2 Papain-like Protease Inhibitors

B Tan, X Liang, A Ansari, P Jadhav, H Tan… - Journal of Medicinal …, 2024 - ACS Publications
The COVID-19 pandemic is caused by SARS-CoV-2, a highly transmissible and pathogenic
RNA betacoronavirus. Like other RNA viruses, SARS-CoV-2 continues to evolve with or …

[HTML][HTML] Mechanistic Insights into Targeting SARS-CoV-2 Papain-like Protease in the Evolution and Management of COVID-19

NN Magwaza, AGA Mushebenge, SC Ugbaja… - BioChem, 2024 - mdpi.com
The COVID-19 pandemic, instigated by the emergence of the novel coronavirus, SARS-CoV-
2, created an incomparable global health crisis. Due to its highly virulent nature, identifying …