PTI-80 / Tasly, ProteoTech - LARVOL DELTA

High-throughput screening of the ReFRAME, Pandemic Box, and COVID Box drug repurposing libraries against SARS-CoV-2 nsp15 endoribonuclease to identify small-molecule inhibitors of viral activity. (PubMed, PLoS One) - "Furthermore, Exebryl-1, a ß-amyloid anti-aggregation molecule for Alzheimer's therapy, was shown to have antiviral activity between 10 to 66 μM, in Vero 76, Caco-2, and Calu-3 cells. Although the inhibitory concentrations determined for Exebryl-1 exceed those recommended for therapeutic intervention, our findings show great promise for further optimization of Exebryl-1 as an nsp15 endoU inhibitor and as a SARS-CoV-2 antiviral."

Journal • Alzheimer's Disease • CNS Disorders • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

[VIRTUAL] Native mass spectrometry supports structure-guided drug discovery for inhibitors of the SARS-CoV-2 non-structural protein 15 (nsp15) (ACS-Sp 2021) - "A gel-based RNA cleavage assay and an in-cell viral inhibition assay further supported the selection of Exebryl-1. Although in vivo delivery is currently a bottleneck to achieve the required concentration for an antiviral effect, Exebryl-1 is a potential template for further optimization via structure-guided drug discovery."

Infectious Disease • Novel Coronavirus Disease • Pain • Respiratory Diseases