Inhibitor screening of proprotein convertases using positional scanning libraries

Proprotein convertases represent an important class of biosynthetic enzymes that are increasingly viewed as targets for therapeutic approaches to infection, cancer, and potentially endocrine disorders. The identification of potent inhibitors can be accomplished by screening synthetic combinatorial libraries containing thousands of small molecules to millions of peptides. In this chapter, the screening of positional scanning libraries is described for the identification of PC1/3 and PC2 inhibitors.