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Updated: Apr 7, 2026

Peptide-based Identification of Functional Motifs and their Binding Partners
Published on: June 30, 2013
Turning Peptide Ligands into Small-Molecule Inhibitors of Protein-Protein Interactions
Chie Hashimoto1, Jutta Eichler1
1Friedrich-Alexander-Universität Erlangen-Nürnberg, Department Chemie und Pharmazie, Schuhstrasse 19, 91052 Erlangen (Germany).
Abstract:
Proline makeover: Truncation and extensive chemical modification of a peptide ligand yielded a biologically active, cell-permeable, peptidomimetic, small-molecule inhibitor of a protein-protein interaction. A key step in this transformation was the replacement of a tetraproline motif by two conformationally constrained diproline units that retain the molecule's PPII helix.
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