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

Autor:	Dolores Díaz, Linda Jütten, Sara Parente, Umberto Piarulli, Lucia Feni, Ines Neundorf
Rok vydání:	2020
Předmět:	Protein Conformation alpha-Helical Cell Survival Peptidomimetic Beta sheet Antineoplastic Agents Stereoisomerism Peptide Cell-Penetrating Peptides Diketopiperazines 01 natural sciences Catalysis 03 medical and health sciences chemistry.chemical_compound Protein structure Materials Chemistry Humans Bifunctional Micelles 030304 developmental biology chemistry.chemical_classification Drug Carriers 0303 health sciences 010405 organic chemistry Chemistry Daunorubicin Metals and Alloys Sodium Dodecyl Sulfate Biological activity General Chemistry 2 5-Diketopiperazine Combinatorial chemistry 0104 chemical sciences 3. Good health Surfaces Coatings and Films Electronic Optical and Magnetic Materials Ceramics and Composites Protein Conformation beta-Strand Peptidomimetics HeLa Cells
Zdroj:	Chemical Communications. 56:5685-5688
ISSN:	1364-548X 1359-7345
DOI:	10.1039/d0cc01490g
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1990d55a4a9e46134cd2a86ded0c576 https://doi.org/10.1039/d0cc01490g Zobrazit plný text záznamu