Mechanisms of Macromolecular Protease Inhibitors

Relatively few design principles underlie the inhibition mechanisms of macromolecular protease inhibitors. These inhibitors tend to compete with substrate binding either through direct competition or deformation of the protease active site; they gain potency and specificity by burying a large surface area and through contacts with specific exosites. Protein engineering has allowed both potency and specificity to be modified.