Thomas Pietschmann - May 12, 2021

Prof. Dr. Thomas Pietschmann, Institute for Experimental Virology, TWINCORE – Center for Experimental and Clinical Infection Research, "Repurposing screen highlighted broad spectrum coronavirus antivirals and their host targets"

The drug repurposing screen has advantages over developing an entirely new drug, such as the lower failure risk, the reduced developmental time frame, and the less cost for investment. Dr. Pietschmann's group joined the coronavirus screen campaigns several months ago. The drug screening started at the 229E-Luc in Huh-7.5 F-Luc cell line, then SARS2 in Calu-3 human lung cell line, and finally authentication with SARS2 in human air-liquid culture. The first screening step inclusion criteria are HCoV 229E virus replication less than 6.5% and cell viability more than 150%. The group has found 12 molecules overlap with the previous screening study and 7 candidates with activity against SARS-CoV-2 in Calu-3 cells. Among the total 134 primary hits passed the first step screening, the 5 CDK inhibitors activity had the highest number of hits (6/54). The reason could be as SARS-CoV-2 regulates CDK activity and viral proteins carry CDK phosphorylation sites. On the other hand, Bardoxolone and Omaveloxolone inhibit SARS-CoV-2 infection of the primary cells as well, while Bardoxolone has entered the SARS-CoV-2 clinical trial an anti-inflammatory tissue-protective compound.