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Proteins, Expression, Isolation and Analysis | … Enzymatic reactions were then started in a black half-volume microplate by addition of 50 μM DABCYL-KTSAVLQSGFRKM-E (EDANS) (GenScript) as a substrate and incubated in … | Get A Quote |
The severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) 3CL protease is a promising target for inhibition of viral replication by interaction with a cysteine residue (Cys145) at its catalytic site. Dalcetrapib exerts its lipid-modulating effect by binding covalently to cysteine 13 of a cholesteryl ester transfer protein. Because 12 free cysteine residues are present in the 3CL protease, we investigated the potential of dalcetrapib to inhibit 3CL protease activity and SARS-CoV-2 replication. Molecular docking investigations suggested that dalcetrapib-thiol binds to the catalytic site of the 3CL protease with a delta value of -8.5 kcal/mol. Dalcetrapib inhibited both 3CL protease activity in vitro and v... More