GRL-0617 | Potent SARS-CoV PLpro inhibitor

GRL-0617 is a potent (IC₅₀ = 600 nM) noncovalent inhibitor of severe acute respiratory syndrome-coronavirus papain-like protease (SARS-CoV PLpro). GRL-0617 inhibited SARS-CoV viral replication in Vero E6 cells with no cytotoxicity (EC₅₀ = 15 µM).  Inactive against human DUB-like proteases HAUSP, USP18, UCH-L1, UCH-L3, and PLP2

References/Citations

1)    Ratia et al. (2008), A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication; Proc. Natl. Acad. Sci. USA, 105 16119

2)    Ghosh et al. (2009), Structure-Based Design, Synthesis, and Biological Evaluation of a Series of Novel and Reversible Inhibitors for the Severe Acute Respiratory Syndrome-Coronavirus Papain-Like Protease; J. Med. Chem. 52 5228