Virtual screening aided in identifying structural leads for viral entry inhibitors of SARS-CoV. Compound 27, which emerged from a 50,240 compound screen and inhibited pseudovirus entry and SARS-CoV plaque formation with EC50 values of 3 mM and 1.6 mM, respectively . A two-step screening of Chinese herbal medicine-based, novel small molecules which bind avidly with the S protein was performed as well. Two virus entry inhibitors, tetra-O-galloyl-p- D-glucose (28) and luteolin (29) were identified and showed anti-SARS-CoV activities with EC50 values of 4.5 and 10.6 mM, respectively .
After binding with ACE2, SARS-CoV is taken up into a vesicle inside the cell. Special cellular enzymes (cathepsins) act in the acidic environment inside the vesicle, facilitating fusion of the viral membrane and the vesicle membrane, so that viral proteins and nucleic acids can enter the cell where viral replication occurs . Thus, the cathepsin L inhibitor, MDL28170 (30) represents an attractive starting point for antiviral therapeutics targeting SARS-CoV entry.
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