Dynamic Amino Acid Side‐Chains Grafting on Folded Peptide Backbone. Issue 36 (19th May 2022)

• Record Type: Journal Article
• Authors: Zagiel, Benjamin; Peker, Taleen; Marquant, Rodrigue; Cazals, Guillaume; Webb, Gabrielle; Miclet, Emeric; Bich, Claudia; Sachon, Emmanuelle; Moumné, Roba
• Is Part Of: Chemistry. Volume 28:Issue 36(2022)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2022-05-19
• Subjects: dynamic combinatorial chemistry -- peptide library -- scaffold grafting; Chemistry -- Periodicals; 540
• DOI: 10.1002/chem.202200454
• Languages: English
• ISSNs: 0947-6539

Abstract

Abstract: An efficient strategy for the synthesis of large libraries of conformationally defined peptides is reported, using dynamic combinatorial chemistry as a tool to graft amino acid side chains on a well‐ordered 3D (3‐dimension) peptide backbone. Combining rationally designed scaffolds with combinatorial side chains selection represents an alternative method to access peptide libraries for structures that are not genetically encodable. This method would allow a breakthrough for the discovery of protein mimetic for unconventional targets for which little is known. Abstract : An efficient access to large libraries of conformationally defined peptides is reported, using dynamic combinatorial chemistry as a tool to graft amino acid's side‐chains in defined arrangement on a well‐ordered 3D peptide scaffold. We report here the design of a chemical system that ensures the scrambling of side‐chains on a pre‐organized scaffold leading to an isoenergetic library useful for ligand screening.