Screening, Synthesis and Biochemical Characterization of SARS-CoV-2 Protease Inhibitors.
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ABSTRACT: The severe acute respiratory syndrome-causing coronavirus 2 (SARS-CoV-2) papain-like protease (PLpro) and main protease (Mpro) play an important role in viral replication events and are important targets for anti-coronavirus drug discovery. In search of these protease inhibitors, we screened a library of 1300 compounds using a fluorescence thermal shift assay (FTSA) and identified 53 hits that thermally stabilized or destabilized PLpro. The hit compounds structurally belonged to two classes of small molecules: thiazole derivatives and symmetrical disulfide compounds. Compound dissociation constants (Kd) were determined using an enzymatic inhibition method. Seven aromatic disulfide compounds were identified as efficient PLpro inhibitors
SUBMITTER: Bagdonas M
PROVIDER: S-EPMC10488051 | biostudies-literature | 2023 Aug
REPOSITORIES: biostudies-literature
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