SARS-CoV-2 M^pro inhibitor identification using a cellular gain-of-signal assay for high-throughput screening.

ABSTRACT: Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2, SARS2) is responsible for the COVID-19 pandemic and infections that continue to affect the lives of millions of people worldwide, especially those who are older and/or immunocompromised. The SARS2 main protease enzyme, M^pro (also called 3C-like protease, 3CL^pro), is a bona fide drug target as evidenced by potent inhibition with nirmatrelvir and ensitrelvir, the active components of the drugs Paxlovid and Xocova, respectively. However, the existence of nirmatrelvir and ensitrelvir-resistant isolates underscores the need to develop next-generation drugs with different resistance profiles and/or distinct mechanisms of action. Here, we report the results of a high-throughput screen of 649,568 compounds using a c

SUBMITTER: Delgado R 

PROVIDER: S-EPMC11550483 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature