Bi-functional radiotheranostics of188 re-liposome-fcy-hegf for radio-and chemo-therapy of egfr-overexpressing cancer cells

Yi Shu Huang, Wei Chuan Hsu, Chien Hong Lin, Sheng Nan Lo, Chu Nian Cheng, Ming Syuan Lin, Te Wei Lee, Chih Hsien Chang*, Keng Li Lan

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

Epidermal growth factor receptor (EGFR) specific therapeutics is of great importance in cancer treatment. Fcy-hEGF fusion protein, composed of yeast cytosine deaminase (Fcy) and human EGF (hEGF), is capable of binding to EGFR and enzymatically convert 5-fluorocytosine (5-FC) to 1000-fold toxic 5-fluorocuracil (5-FU), thereby inhibiting the growth of EGFR-expressing tumor cells. To develop EGFR-specific therapy,188Re-liposome-Fcy-hEGF was constructed by insertion of Fcy-hEGF fusion protein onto the surface of liposomes encapsulating of188Re. Western blotting, MALDI-TOF, column size exclusion and flow cytometry were used to confirm the con-jugation and bio-activity of188Re-liposome-Fcy-hEGF. Cell lines with EGFR expression were subjected to treat with 188 Re-liposome-Fcy-hEGF/5-FC in the presence of 5-FC. The 188 Re-liposome-Fcy-hEGF/5-FC revealed a better cytotoxic effect for cancer cells than the treatment of liposome-Fcy-hEGF/5-FC or188Re-liposome-Fcy-hEGF alone. The therapeutics has radio-and chemo-toxicity simultaneously and specifically target to EGFR-expression tumor cells, thereby achieving synergistic anticancer activity.

Original languageEnglish
Article number1902
Pages (from-to)1-12
Number of pages12
JournalInternational Journal Of Molecular Sciences
Volume22
Issue number4
DOIs
StatePublished - 2 Feb 2021

Keywords

  • 5-fluorocuracil
  • Cytosine deaminase
  • Epidermal growth factor receptor
  • Liposome
  • Pro-drug
  • Rhenium-188

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