Scientists identify papain-like protease inhibitor against COVID-19 biorxivpreprint UCLA SARSCoV2 COVID19 Coronavirus ProteinInhibitor
By Bhavana KunkalikarJul 25 2022Reviewed by Aimee Molineux In a recent study posted to the bioRxiv* preprint server, researchers identified a papain-like protease inhibitor for treating severe acute respiratory syndrome coronavirus 2 infections.
The team assessed small molecules from a custom clinical library comprising 58 compounds that were collected from different sources based on their inhibitory activity against the PLpro enzyme. The effectiveness of the inhibitors against PLpro was analyzed by estimating the dose-response inhibition of PLpro along with its deISGylase and deubiquitinase activities. Furthermore, the team assessed whether PLpro inhibitors could rescue interferon-beta induction.
Related StoriesValidation of DDL-701 inhibitory activity against PLpro showed that the IC50 value for the dose-response inhibition of PLpro was 13 μM, the deubiquitinase activity was 21 μM and the deISGylase activity was 8 μM. Moreover, the dose-response curves generated for DDL-713, DDL-715, and GRL-0617 revealed weaker inhibitory potency as compared to that of DDL-701.
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