title: Peptide scanning for studying structure-activity relationships in drug discovery.
abstract: Peptide-based therapeutics have grown in importance over the last few decades. Furthermore, peptides have been extensively used as lead compounds in the drug discovery process to investigate the nature of chemical space required for molecular recognition and activity at a variety of targets. This critical commentary reviews scanning techniques, which employ natural and non-proteinogenic amino acids to facilitate understanding of structural requirements for peptide biological activity. The value of sequence analysis by such methods is highlighted by examples, in which the elements for peptide affinity and activity have been elucidated and employed to prepare peptidomimetic leads for drug development.
authors.affiliation: Department of Chemistry, University of Leicester, Leicester LE1 7RH, UK.
authors.forename: Andrew G
authors.initials: AG
authors.lastname: Jamieson
authors.forename: Nicolas
authors.initials: N
authors.lastname: Boutard
authors.forename: David
authors.initials: D
authors.lastname: Sabatino
authors.forename: William D
authors.initials: WD
authors.lastname: Lubell
mesh_terms: D000596:Amino Acids / Q000737:chemistry; D001372:Aza Compounds / Q000737:chemistry; D015195:Drug Design; D007769:Lactams / Q000737:chemistry; D010455:Peptides / Q000737:chemistry*; D057786:Peptidomimetics; D017433:Protein Structure, Secondary; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D001372:Aza Compounds; D007769:Lactams; D010455:Peptides; D057786:Peptidomimetics