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Computed Tomography-guided Time-domain Diffuse Fluorescence Tomography in Small Animals for Localization of Cancer Biomarkers
Published on: July 17, 2012
A biotin-guided fluorescent-peptide drug delivery system for cancer treatment
Taeyoung Kim1, Hyun Mi Jeon, Hoa Thi Le
1Department of Chemistry, Korea University, Seoul 136-701, Korea. jongskim@korea.ac.kr.
Abstract:
Herein, we present a fluorescent-peptide drug delivery system composed of biotin-naphthalimide-HJ inhibitor peptide2, prodrug 1. Treatment of 1 to biotin receptor-positive HepG2 cells, which are resistant to high concentrations of the HJ inhibitor peptide2, decreased cell viability and increased intracellular fluorescence.
Insights
A novel fluorescent-peptide drug delivery system effectively targeted biotin receptor-positive cancer cells. This system, prodrug 1, reduced cancer cell viability and enhanced intracellular fluorescence, overcoming resistance to the HJ inhibitor peptide2.
Area of Science:
- Biochemistry
- Drug Delivery
- Molecular Biology
Background:
- Hepatocellular carcinoma (HCC) poses a significant health challenge.
- Targeted drug delivery systems are crucial for overcoming cancer cell resistance.
- Biotin receptors are overexpressed on certain cancer cells, presenting a therapeutic target.
Purpose of the Study:
- To develop and evaluate a novel fluorescent-peptide drug delivery system for targeting biotin receptor-positive cancer cells.
- To assess the efficacy of the developed system in reducing cancer cell viability.
- To investigate the intracellular fluorescence enhancement upon drug delivery.
Main Methods:
- Synthesis of a fluorescent-peptide prodrug (prodrug 1) incorporating biotin, naphthalimide, and HJ inhibitor peptide2.
- Treatment of biotin receptor-positive HepG2 cells with prodrug 1.
- Assessment of cell viability using standard assays.
- Measurement of intracellular fluorescence.
Main Results:
- Prodrug 1 demonstrated targeted delivery to biotin receptor-positive HepG2 cells.
- Treatment with prodrug 1 significantly decreased HepG2 cell viability.
- Intracellular fluorescence was markedly increased following treatment with prodrug 1, indicating successful drug delivery.
- The system overcame resistance to high concentrations of HJ inhibitor peptide2.
Conclusions:
- The developed fluorescent-peptide drug delivery system shows promise for targeted cancer therapy.
- Prodrug 1 effectively targets and reduces viability of biotin receptor-positive cancer cells.
- This system offers a potential strategy for overcoming drug resistance in cancer treatment.

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