title: Inhibitor screening of proprotein convertases using positional scanning libraries.
abstract: 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.
authors.affiliation: School of Medicine Anatomy and Neurobiology, University of Maryland-Baltimore, Baltimore, MD 21201, USA. ilind001@umaryland.edu
authors.forename: Iris
authors.initials: I
authors.lastname: Lindberg
authors.forename: Jon R
authors.initials: JR
authors.lastname: Appel
mesh_terms: D000595:Amino Acid Sequence; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D004700:Endocrine System Diseases / Q000201:enzymology; D057166:High-Throughput Screening Assays / Q000379:methods*; D006801:Humans; D007239:Infections / Q000201:enzymology; D009369:Neoplasms / Q000201:enzymology; D019151:Peptide Library; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology; D043484:Proprotein Convertases / Q000037:antagonists & inhibitors*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D054852:Small Molecule Libraries
chemical_list: D019151:Peptide Library; D010455:Peptides; D011480:Protease Inhibitors; D054852:Small Molecule Libraries; D043484:Proprotein Convertases