title: Selection-based discovery of macrocyclic peptides for the next generation therapeutics.
abstract: Naturally occurring macrocyclic peptides represent a unique class of compounds that exhibit various biological activities ranging from antibiotics to immunosuppressant. Although the discovery of such macrocyclic peptides had relied on their isolation from living organisms, recent advances in ribosomal peptide synthesis and in display techniques made it possible to use artificially generated macrocyclic peptide libraries for selection of ligands for biologically relevant proteins. In this review, we discuss the technologies and their applications for the discovery of peptide ligands.
authors.affiliation: Department of Chemistry, Graduate School of Science, The University of Tokyo, Tokyo 113-0033, Japan.
authors.forename: Tomomi
authors.initials: T
authors.lastname: Morioka
authors.affiliation: Department of Chemistry, Graduate School of Science, The University of Tokyo, Tokyo 113-0033, Japan.
authors.forename: Nikita D
authors.initials: ND
authors.lastname: Loik
authors.affiliation: Department of Chemistry, Graduate School of Science, The University of Tokyo, Tokyo 113-0033, Japan.
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Hipolito
authors.affiliation: Department of Chemistry, Graduate School of Science, The University of Tokyo, Tokyo 113-0033, Japan.
authors.forename: Yuki
authors.initials: Y
authors.lastname: Goto
authors.affiliation: Department of Chemistry, Graduate School of Science, The University of Tokyo, Tokyo 113-0033, Japan; CREST, JST, Tokyo 113-0033, Japan. Electronic address: hsuga@chem.s.u-tokyo.ac.jp.
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Suga
mesh_terms: D003500:Cyclization; D055808:Drug Discovery; D020869:Gene Expression Profiling / Q000379:methods; D006801:Humans; D006842:Hydrocarbons, Brominated / Q000737:chemistry; D008024:Ligands; D008958:Models, Molecular; D019151:Peptide Library; D010456:Peptides, Cyclic / Q000096:biosynthesis / Q000737:chemistry / Q000302:isolation & purification*; D014176:Protein Biosynthesis; D012270:Ribosomes / Q000235:genetics; D056565:Sirtuin 2 / Q000037:antagonists & inhibitors / Q000737:chemistry; D013388:Succinimides / Q000737:chemistry
chemical_list: D006842:Hydrocarbons, Brominated; D008024:Ligands; D019151:Peptide Library; D010456:Peptides, Cyclic; D013388:Succinimides; C525695:alpha,alpha'-dibromoxylene; C096464:disuccinimidyl glutarate; C474199:SIRT2 protein, human; D056565:Sirtuin 2