Bi-Functional Peptides as a New Therapeutic Tool for Hepatocellular Carcinoma.

Abstract

BACKGROUND:

The interfering peptides that block protein-protein interactions have been receiving increasing attention as potential therapeutic tools.

METHODS:

We measured the internalization and biological effect of four bi-functional tumor-penetrating and interfering peptides into primary hepatocytes isolated from three non-malignant and 11 hepatocellular carcinomas.

RESULTS:

These peptides are internalized in malignant hepatocytes but not in non-malignant cells. Furthermore, the degree of peptide internalization correlated with receptor expression level and tumor aggressiveness levels. Importantly, penetration of the peptides iRGD-IP, LinTT1-IP, TT1-IP, and RPARPAR-IP induced apoptosis of the malignant hepatocytes without effect on non-malignant cells.

CONCLUSION:

Receptor expression levels correlated with the level of peptide internalization and aggressiveness of the tumor. This study highlights the potential to exploit the expression of tumor-penetrating peptide receptors as a predictive marker of liver tumor aggressiveness. These bi-functional peptides could be developed for personalized tumor treatment.

• Authors: Eric Savier, Lorena Simon-Gracia, Frederic Charlotte, Pierre Tuffery, Tambet Teesalu, Olivier Scatton, Angelita Rebollo
• Journal: Pharmaceutics (Pharmaceutics) Vol. 13 Issue 10 (Oct 06 2021) ISSN: 1999-4923 [Print] Switzerland
• PMID: 34683924 (Publication Type: Journal Article)