Protease inhibitor: SARS-CoV papain-like protease (PLpro, Nsp3). Inhibits SARS-CoV in cells, likely also inhibits SARS-CoV-2, whose Nsp3 has 87% similarity overall to that of SARS-CoV. Shanker et al. ChemRxiv, Mar 4 2020, http://doi.org/10.26434/chemrxiv.11846943.v7; Gordon et al. Nature, Apr 30 2020, https://doi.org/10.1038/s41586-020-2286-9.
Biochemicals & reagents
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
GRL-0617 is a potent (IC50 = 600 nM) noncovalent inhibitor of severe acute respiratory syndrome-coronavirus papain-like protease (SARS-CoV PLpro). This compound inhibited SARS-CoV viral replication in Vero E6 cells with no cytotoxicity (EC50 = 15 µM) but is inactive against human DUB-like proteases HAUSP, USP18, UCH-L1, UCH-L3, and PLP2.