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

hepatocellular carcinoma interfering peptides tumor-penetrating peptides

Journal

Pharmaceutics
ISSN: 1999-4923
Titre abrégé: Pharmaceutics
Pays: Switzerland
ID NLM: 101534003

Informations de publication

Date de publication:
06 Oct 2021
Historique:
received: 06 09 2021
revised: 29 09 2021
accepted: 30 09 2021
entrez: 23 10 2021
pubmed: 24 10 2021
medline: 24 10 2021
Statut: epublish

Résumé

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

Sections du résumé

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

Identifiants

pubmed: 34683924
pii: pharmaceutics13101631
doi: 10.3390/pharmaceutics13101631
pmc: PMC8541685
pii:
doi:

Types de publication

Journal Article

Langues

eng

Subventions

Organisme : Inserm
ID : 2018
Organisme : European Regional Development Fund
ID : 2014-2020.4.01.15-0012
Organisme : Estonian Research Council
ID : PRG230 and EAG79

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Auteurs

Eric Savier (E)

Department of Hepatobiliary and Liver Transplantation Surgery, AP-HP, Pitié-Salpêtrière Hospital, Sorbonne Université, 75006 Paris, France.
Sant Antoine Research Center (CRSA), Institut Nationale de la Santé et la Recherche Médicale (Inserm), Institute of Cardiometabolism and Nutrition (ICAN), Sorbonne Université, 75006 Paris, France.

Lorena Simon-Gracia (L)

Laboratory of Precision and Nanomedicine, Institute of Biomedicine and Translational Medicine, University of Tartu, 50090 Tartu, Estonia.

Frederic Charlotte (F)

Department of Pathology, AP-HP, Pitié-Salpêtrière Hospital, 75006 Paris, France.

Pierre Tuffery (P)

Biologie Fontionelle Adaptative (BFA), Unité Mixte de Recherche (UMR) 8251, Centre National de la Recherche Scientifique (CNRS) ERL U1133, Inserm, Université de Paris, 75006 Paris, France.

Tambet Teesalu (T)

Laboratory of Precision and Nanomedicine, Institute of Biomedicine and Translational Medicine, University of Tartu, 50090 Tartu, Estonia.
Center for Nanomedicine and Department of Cell, Molecular and Developmental Biology, University of California, Santa Barbara, CA 93106, USA.

Olivier Scatton (O)

Department of Hepatobiliary and Liver Transplantation Surgery, AP-HP, Pitié-Salpêtrière Hospital, Sorbonne Université, 75006 Paris, France.
Sant Antoine Research Center (CRSA), Institut Nationale de la Santé et la Recherche Médicale (Inserm), Institute of Cardiometabolism and Nutrition (ICAN), Sorbonne Université, 75006 Paris, France.

Angelita Rebollo (A)

Faculté de Pharmacie, Unité des Technologies Chimiques et Biologiques pour la Santé (UTCBS), Inserm U1267, Centre National de la Recherche Scientifique CNRS UMR8258, Université de Paris, 75006 Paris, France.

Classifications MeSH