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. 2022 Jun 27;28(36):e202200454.
doi: 10.1002/chem.202200454. Epub 2022 May 19.

Dynamic Amino Acid Side-Chains Grafting on Folded Peptide Backbone

Benjamin Zagiel  1 , Taleen Peker  1 , Rodrigue Marquant  1 , Guillaume Cazals  2 , Gabrielle Webb  1 , Emeric Miclet  1 , Claudia Bich  2 , Emmanuelle Sachon  1   3 , Roba Moumné  1
Affiliations

Dynamic Amino Acid Side-Chains Grafting on Folded Peptide Backbone

Benjamin Zagiel et al. Chemistry. .

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.

Keywords: dynamic combinatorial chemistry; peptide library; scaffold grafting.

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