Repurposing screen highlights broad-spectrum coronavirus antivirals and their host targets
S. Haid, A. Matthaei, M. Winkler, S. M. Sake, A. P. Gunesch, J. Rueckert, G. Vieyres, D. Kuehl, T.-T. Nguyen, L. Lasswitz, F. Zapatero, G. Brogden, G. Gerold, B. Wiegmann, U. Bilitewski, M. Broenstrup, T. Schulz, T. Pietschmann
Abstract
Libraries composed of licensed drugs represent a vast repertoire of molecules modulating physiologic processes in humans, thus providing unique opportunities for discovery of host targeting antivirals. We interrogated the ReFRAME repurposing library with 12,993 molecules for broad-spectrum coronavirus antivirals and discovered 134 compounds inhibiting an alphacoronavirus, mapping to 59 molecular target categories. Dominant targets included the 5-hydroxytryptamine receptor and dopamine receptor and cyclin-dependent kinase inhibitors. Counter-screening with SARS-CoV-2 and validation in primary cells identified Phortress, an aryl hydrocarbon receptor (AHR) ligand, Bardoxolone and Omaveloxolone, two nuclear factor, erythroid 2 like 2 (NFE2L2) activators as inhibitors of both alpha- and betacoronaviruses. The landscape of coronavirus targeting molecules provides important information for the development of broad-spectrum antivirals reinforcing pandemic preparedness.
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