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Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
Published on: April 25, 2025
Bi-Functional Peptides as a New Therapeutic Tool for Hepatocellular Carcinoma
Eric Savier1,2, Lorena Simon-Gracia3, Frederic Charlotte4
1Department of Hepatobiliary and Liver Transplantation Surgery, AP-HP, Pitié-Salpêtrière Hospital, Sorbonne Université, 75006 Paris, France.
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.
Insights
Bi-functional peptides target malignant liver cells, not healthy ones, by blocking protein-protein interactions. Their uptake correlates with tumor aggressiveness, offering potential for personalized liver cancer treatment.
Area of Science:
- Biochemistry
- Oncology
- Drug Delivery
Background:
- Interfering peptides that block protein-protein interactions are emerging as significant therapeutic agents.
- Targeting specific cellular interactions is crucial for developing effective cancer therapies.
Purpose of the Study:
- To evaluate the internalization and biological impact of four bi-functional peptides in liver cancer cells.
- To assess the correlation between peptide uptake, receptor expression, and tumor aggressiveness.
Main Methods:
- Primary hepatocytes from non-malignant and hepatocellular carcinoma (HCC) tissues were used.
- Four bi-functional tumor-penetrating and interfering peptides (iRGD-IP, LinTT1-IP, TT1-IP, RPARPAR-IP) were tested for internalization and biological effects.
Main Results:
- Peptides were internalized by malignant hepatocytes but not by non-malignant cells.
- Peptide internalization levels correlated with receptor expression and tumor aggressiveness.
- Peptide penetration induced apoptosis in malignant hepatocytes without affecting non-malignant cells.
Conclusions:
- Receptor expression levels predict peptide internalization and liver tumor aggressiveness.
- Tumor-penetrating peptide receptors may serve as predictive markers for liver cancer.
- These bi-functional peptides show promise for personalized liver cancer treatment strategies.
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