From peptides to drugs via phage display

• Published in: Drug discovery today Vol. 3; no. 8; pp. 370 - 378
• Main Authors: Kay, Brian K., Kurakin, Alexei V., Hyde-DeRuyscher, Robin
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01-08-1998; Elsevier Science
• Subjects: Biological and medical sciences; combinatorial chemistry; General pharmacology; high-throughput screening; Medical sciences; peptidomimetics; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; protein–protein interaction; target validation; protein–protein interaction; peptidomimetics; combinatorial chemistry; target validation; high-throughput screening; Virus; Drug; Pharmaceutical technology; Targeting; Peptides; Peptidomimetic compound; Review; Molecular biology; Research and development; Phage
• ISSN: 1359-6446; 1878-5832
• DOI: 10.1016/S1359-6446(98)01220-3

In the past ten years, there has been a flurry of research generating and screening combinatorial peptide libraries. Molecular biologists have favored phage display as a means of generating millions to billions of different peptides for the purposes of mapping protein–protein interactions of antibodies, cell surface receptors and intracellular proteins. This article summarizes recent work on identifying peptide ligands via phage display and several methods by which they serve to promote drug discovery: design of peptidomimetics, biological validation of targets, and the establishment of high-throughput screens of chemical compound libraries. These methods provide powerful aids in the search for lead compounds of previously `unscreenable' targets and for new targets discovered in genomics efforts.