Induced‐Fit Binding of the Macrocyclic Noncovalent Inhibitor TMC435 to its HCV NS3/NS4A Protease Target

This is the authors' abstract. We don't add key points for this paper.

If the shoe fits: TMC435, a noncovalent small-molecule inhibitor of the hepatitis C virus (HCV) NS3/NS4A protease, is currently undergoing clinical evaluation as an HCV therapeutic. In the crystal structure of the noncovalent NS3/NS4A protease–TMC435 complex the bound inhibitor exploits induced-fit binding. The new structure is consistent with the emerging view of viral resistance to NS3/NS4A protease inhibitors.