Cell-penetrating peptides containing 2, 5-diketopiperazine (DKP) scaffolds as shuttles for anti-cancer drugs: conformational studies and biological activity. Issue 42 (22nd April 2020)

• Record Type: Journal Article
• Authors: Feni, Lucia; Jütten, Linda; Parente, Sara; Piarulli, Umberto; Neundorf, Ines; Diaz, Dolores
• Is Part Of: Chemical communications. Volume 56:Issue 42(2020)
• Page Start: 5685
• Page End: 5688
• Publication Date: 2020-04-22
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d0cc01490g
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : Cargo-peptides approaching cellular membranes: influence of cyclization and stereochemistry on cellular translocation activity of a novel group of cell-penetrating peptides containing bifunctional diketopiperazine. Abstract : A series of linear and cyclic peptidomimetics composed of a cell-penetrating peptide and a non-natural, bifunctional 2, 5-diketopiperazine scaffold is reported. Conformational studies revealed well-defined helical structures in micellar medium for linear structures, while cyclic peptidomimetics were more flexible. Biological investigations showed higher membrane-activity of cyclic derivatives allowing their use as shuttles for anti-cancer drugs.