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Updated: May 27, 2026

Evaluation of the In vivo Antitumor Activity of Polyanhydride IL-1α Nanoparticles
Published on: June 28, 2021
Targeting interleukin-4 receptor α with hybrid peptide for effective cancer therapy
Liying Yang1, Tomohisa Horibe, Masayuki Kohno
1Department of Pharmacoepidemiology, Graduate School of Medicine and Public Health, Kyoto University, Yoshidakonoe-cho, Sakyo-ku, Kyoto, Japan.
Abstract:
Interleukin-4 receptor α (IL-4Rα) chain is highly expressed on the surface of various human solid tumors. We designed a novel hybrid peptide termed IL-4Rα-lytic peptide that targets the IL-4Rα chain. The IL-4Rα-lytic peptide contains a target moiety to bind to IL-4Rα and a cellular toxic lytic peptide that selectively kills cancer cells. The anticancer activity of the IL-4Rα-lytic peptide was evaluated in vitro and in vivo. It was found that the IL-4Rα-lytic peptide has cytotoxic activity in cancer cell lines expressing IL-4Rα, determined by quantitative real-time PCR. The IC(50) ratios of the lytic peptide to the IL-4Rα-lytic peptide correlated well with the expression levels of IL-4Rα on cancer cells (r = 0.80). In addition, IL-4Rα-lytic peptide administered either intratumoraly or intravenously significantly inhibited tumor growth in xenograft model of human pancreatic cancer (BXPC-3) in mice. These results indicate that the IL-4Rα-lytic peptide generated in this study has a potent and selective anticancer potential against IL-4Rα-positive solid cancers.
Insights
A novel hybrid peptide selectively targets and kills Interleukin-4 receptor α (IL-4Rα)-positive cancer cells. This peptide shows potent anticancer activity in vitro and significantly inhibits tumor growth in vivo, offering a promising new cancer therapy.
Area of Science:
- Oncology
- Molecular Biology
- Biotechnology
Background:
- Interleukin-4 receptor α (IL-4Rα) is overexpressed on many human solid tumors.
- Targeting IL-4Rα presents a potential strategy for selective cancer therapy.
Purpose of the Study:
- To design and evaluate a novel hybrid peptide, IL-4Rα-lytic peptide, for targeted cancer treatment.
- To assess the in vitro and in vivo anticancer efficacy of the IL-4Rα-lytic peptide.
Main Methods:
- Quantitative real-time PCR to determine IL-4Rα expression levels.
- In vitro cytotoxicity assays on cancer cell lines.
- In vivo studies using a human pancreatic cancer xenograft mouse model.
Main Results:
- IL-4Rα-lytic peptide demonstrated significant cytotoxic activity against IL-4Rα-expressing cancer cells.
- A strong correlation (r = 0.80) was observed between IL-4Rα expression levels and peptide efficacy.
- Intratumoral and intravenous administration of the peptide significantly inhibited tumor growth in mice.
Conclusions:
- The designed IL-4Rα-lytic peptide exhibits potent and selective anticancer potential.
- This hybrid peptide is a promising candidate for treating IL-4Rα-positive solid tumors.
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