99mTc-radiolabeled GE11-modified peptide for ovarian tumor targeting

Daru. 2017 May 2;25(1):13. doi: 10.1186/s40199-017-0179-8.

Abstract

Background: Ovarian cancer is a serious threat for women health and the early diagnosis of this cancer might improves the survival rate of patients. The use of the targeted radiopharmaceuticals could be a non-invasive and logical method for tumor imaging. The aim of this study was to radiolabel GE11 peptide as a new specific probe for imaging of ovarian tumor.

Methods: HYNIC-SSS-GE11 peptide was labeled with 99mTc using tricine as a coligand. The 99mTc-tricine-HYNIC-SSS-GE11 peptide was evaluated for specific cellular binding in three cell lines with different levels of EGFR expression. Tumor targeting was assessed in SKOV3 tumor bearing mice.

Results: By using tricine as a coligand, labeling yield was more than 98% and the stability of the radiolabelled peptide in human serum up to 4 h was 96%. The in vitro cell uptake test showed that this radiolabeled peptide had a good affinity to SKOV3 cells with dissociation constant of 73 nM. The in vivo results showed a tumor/muscle ratio of 3.2 at 4 h following injection of 99mTc-tricine-HYNIC-SSS-GE11 peptide.

Conclusions: Results of this study showed that 99mTc-tricine-HYNIC-SSS-GE11 peptide could be a promising tool for diagnosis and staging of ovarian cancer. 99mTc-tricine-HYNIC-SSS-GE11, a novl targeted agent for ovarian tumor imaging.

Keywords: 99mTc; GE11 peptide; HYNIC; Molecular imaging; Radiopharmaceuticals.

MeSH terms

  • Animals
  • Female
  • Humans
  • MCF-7 Cells
  • Mice
  • Mice, Nude
  • Neoplasm Transplantation
  • Ovarian Neoplasms / diagnostic imaging*
  • Ovarian Neoplasms / metabolism
  • Peptides / metabolism
  • Peptides / therapeutic use*
  • Radiopharmaceuticals / therapeutic use
  • Technetium / therapeutic use
  • Tissue Distribution

Substances

  • GE11 peptide
  • Peptides
  • Radiopharmaceuticals
  • Technetium