Development of a Fluorescence Polarization Assay for the SARS-CoV-2 Papain-like Protease.

ABSTRACT: The COVID-19 pandemic has caused significant losses to the global community. Although effective vaccination and antiviral therapeutics provide primary defense, SARS-CoV-2 remains a public health threat, given the emerging resistant variants. The SARS-CoV-2 papain-like protease (PL^pro) is essential for viral replication and is a promising drug target. We recently designed a series of biarylphenyl PL^pro inhibitors with a representative lead Jun12682 showing potent antiviral efficacy in a SARS-CoV-2 infection mouse model. In this study, we designed a fluorescein-labeled biarylphenyl probe Jun12781 and used it to optimize a fluorescence polarization (FP) assay. The FP assay is suitable for high-throughput screening with a Z' factor of 0.69. In additio

SUBMITTER: Li K 

PROVIDER: S-EPMC11915184 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature