Identification of a peptide for folate receptor alpha by phage display and its tumor targeting activity in ovary cancer xenograft

Sci Rep. 2018 May 30;8(1):8426. doi: 10.1038/s41598-018-26683-z.

Abstract

The expression level of folate receptor alpha (FRα) is located highly rate in ovarian cancer though it is remained absent in normal tissues. This highly tumor restricted expression profile makes FRα a promising target for tumor therapy and diagnosis. In this research we report a FRα binding peptide C7(Met-His-Thr-Ala-Pro-Gly-Trp-Gly-Tyr-Arg-Leu-Ser) discovered by phage display and this peptide showed specific binding to FRα expressing cells by cell ELISA and flow cytometry. Tumor targeting ability of C7 was proved in vivo by both phage homing experiment and fluorescence imaging. C7 can be internalized by SKOV3 cells and its affinity to FRα was determined by MST. The molecular recognition was revealed by structure modeling, suggesting its binding mode with FRα.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Cell Line, Tumor
  • Cell Surface Display Techniques*
  • Female
  • Folate Receptor 1 / chemistry
  • Folate Receptor 1 / metabolism*
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Mice
  • Molecular Docking Simulation
  • Molecular Targeted Therapy*
  • Ovarian Neoplasms / drug therapy
  • Ovarian Neoplasms / metabolism
  • Ovarian Neoplasms / pathology*
  • Peptide Hydrolases / chemistry
  • Peptide Hydrolases / metabolism
  • Peptide Hydrolases / pharmacology*
  • Protein Structure, Secondary
  • Protein Transport / drug effects
  • Xenograft Model Antitumor Assays*

Substances

  • Folate Receptor 1
  • Peptide Hydrolases
  • oligopeptidase