Author/Authors :
Cristina Rosés، نويسنده , , Daniel Carbajo، نويسنده , , Gl?ria Sanclimens، نويسنده , , Josep Farrera-Sinfreu، نويسنده , , Adriana Blancafort، نويسنده , , Gl?ria Oliveras، نويسنده , , Anna D. Cirac، نويسنده , , Eduard Bardaj?، نويسنده , , Teresa Puig، نويسنده , , Marta Planas، نويسنده , , Lidia Feliu، نويسنده , , Fernando Albericio، نويسنده , , Miriam Royo and Maria J. Macias، نويسنده ,
Abstract :
In this study, we combined a cell-penetrating γ-peptide, PEG-1, with antimicrobial undecapeptides in order to provide compounds with anticancer properties against MDA-MB-231 human breast cancer cells. We demonstrated that the conjugates were more cytotoxic than Ac-PEG-1 and the parent undecapeptides. We also evaluated the toxicity of the conjugates against non-malignant cells. The peptide conjugate with the best biological profile was BP77-PEG-1, which, at 10 μM, showed a 71% growth inhibition in MDA-MB-231 cells and only a 17% inhibition in non-malignant cells. Therefore, this study suggests that PEG-1 mediated the undecapeptide delivery into cancer cells and that these conjugates are the proof-of-concept of this strategy to generate improved anticancer drugs based on peptides.
Keywords :
Cell-penetrating peptides , Antimicrobial peptides , Foldamers , Anticancer , ?-Peptides
