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Updated: May 2, 2026
Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
Published on: December 1, 2020
Selection-based discovery of druglike macrocyclic peptides
Toby Passioura1, Takayuki Katoh, Yuki Goto
1Department of Chemistry, Graduate School of Science, University of Tokyo, Tokyo 113-0033, Japan; email: toby@chem.s.u-tokyo.ac.jp , katoh@chem.s.u-tokyo.ac.jp , y-goto@chem.s.u-tokyo.ac.jp , hsuga@chem.s.u-tokyo.ac.jp.
Abstract:
Macrocyclic peptides are an emerging class of therapeutics that can modulate protein-protein interactions. In contrast to the heavily automated high-throughput screening systems traditionally used for the identification of chemically synthesized small-molecule drugs, peptide-based macrocycles can be synthesized by ribosomal translation and identified using in vitro selection techniques, allowing for extremely rapid (hours to days) screening of compound libraries comprising more than 10(13) different species. Furthermore, chemical modification of translated peptides and engineering of the genetic code have greatly expanded the structural diversity of the available peptide libraries. In this review, we discuss the use of these technologies for the identification of bioactive macrocyclic peptides, emphasizing recent developments.
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