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

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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.

Graphical abstract: Cell-penetrating peptides containing 2,5-diketopiperazine (DKP) scaffolds as shuttles for anti-cancer drugs: conformational studies and biological activity

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Article information


Submitted
25 Feb 2020
Accepted
15 Apr 2020
First published
16 Apr 2020

Chem. Commun., 2020,56, 5685-5688
Article type
Communication

Cell-penetrating peptides containing 2,5-diketopiperazine (DKP) scaffolds as shuttles for anti-cancer drugs: conformational studies and biological activity

L. Feni, L. Jütten, S. Parente, U. Piarulli, I. Neundorf and D. Diaz, Chem. Commun., 2020, 56, 5685
DOI: 10.1039/D0CC01490G

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