CHEMICAL MODIFICATIONS AND ANTI-PROLIFERATIVE ACTIVITY OF A BI-FUNCTIONAL PEPTIDE AGAINST MDA-MB-231 BREAST CANCER CELLS.

AVPI-(Ala-Val-Pro-Ile) and RGD-(Arg-Gly-Asp) peptides have recently attracted a growing interest in the anticancer drug design and development. Following the concept of combining two fragments with different functionalities in order to achieve increased effects, we present herein the synthesis of two AVPI-RGD peptides. The impact of the performed chemical modifications on the anti-proliferative activity of these peptides was evaluated at MDA-MB-231 cancer cells. It was found that the conjugated peptide with modifications at proline and arginine residues showed a higher anti-proliferative effect than the parent AVPI-RGD molecule. Furthermore, it was observed that the effect of AVHypI-AgbGD vs. that of its co-administrated structural subunits was higher. The results obtained in this work suggested that the introduced substitutions and the conjugation of the two functional motifs benefit the anti-proliferative activity of the parent peptides. [ABSTRACT FROM AUTHOR]