title: Methods for the creation of cyclic Peptide libraries for use in lead discovery.
abstract: The identification of initial hits is a crucial stage in the drug discovery process. Although many projects adopt high-throughput screening of small-molecule libraries at this stage, there is significant potential for screening libraries of macromolecules created using chemical biology approaches. Not only can the production of the library be directly interfaced with a cell-based assay, but these libraries also require significantly fewer resources to generate and maintain. In this context, cyclic peptides are increasingly viewed as ideal scaffolds and have proven capability against challenging targets such as protein-protein interactions. Here we discuss a range of methods used for the creation of cyclic peptide libraries and detail examples of their successful implementation.
authors.affiliation: Chemistry, University of Southampton, Southampton, UK.
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Foster
authors.affiliation: Chemistry, University of Southampton, Southampton, UK.
authors.forename: James D
authors.initials: JD
authors.lastname: Ingram
authors.affiliation: Chemistry, University of Southampton, Southampton, UK.
authors.forename: Eilidh K
authors.initials: EK
authors.lastname: Leitch
authors.affiliation: Chemistry, University of Southampton, Southampton, UK.
authors.forename: Katherine R
authors.initials: KR
authors.lastname: Lennard
authors.affiliation: Chemistry, University of Southampton, Southampton, UK.
authors.forename: Eliot L
authors.initials: EL
authors.lastname: Osher
authors.affiliation: Chemistry, University of Southampton, Southampton, UK Cancer Sciences, University of Southampton, Southampton, UK a.tavassoli@soton.ac.uk.
authors.forename: Ali
authors.initials: A
authors.lastname: Tavassoli
mesh_terms: D061505:Cell Surface Display Techniques; D055808:Drug Discovery / Q000379:methods*; D066298:In Vitro Techniques; D019151:Peptide Library; D010456:Peptides, Cyclic; D014176:Protein Biosynthesis
chemical_list: D019151:Peptide Library; D010456:Peptides, Cyclic
keywords: cyclic peptide; high-throughput screening; protein-protein interactions; review