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June 24, 2021

'Bispecific repurposed medicines targeting the viral and immunological arms of COVID-19', published in nature scientific reports

Our paper, 'Bispecific repurposed medicines targeting the viral and immunological arms of COVID-19', is now out in nature scientific reports. Protecting against future outbreaks requires targets conserved between coronavirus strains and amenable to drug discovery. We identified two non-antiviral therapeutic agents, the caspase-1 inhibitor SDZ 224015 and Tarloxotinib that target Mpro and PLpro, respectively through extensive experimental screens of the drug repurposing ReFRAME library of 12,000 therapeutic agents. Caspase-1 inhibitor SDZ 224015, was found to be a potent irreversible inhibitor of Mpro (IC50 30 nM) while Tarloxotinib, a clinical stage epidermal growth factor receptor inhibitor, is a sub micromolar inhibitor of PLpro (IC50 300 nM, Ki 200 nM) and is the first reported PLpro inhibitor with drug-like properties. SDZ 224015 and Tarloxotinib have both already undergone safety evaluation in humans. Read the full Open Access paper through the following link; https://www.nature.com/articles/s41598-021-92416-4