Related Experiment Video

Updated: Jan 31, 2026

Preparing a 68Ga-labeled Arginine Glycine Aspartate RGD-peptide for Angiogenesis
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Preparing a 68Ga-labeled Arginine Glycine Aspartate RGD-peptide for Angiogenesis

Published on: January 7, 2019

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68Ga-labelled NOTA-RGD-GE11 peptide for dual integrin and EGFR-targeted tumour imaging

Chien-Jen Chen1, Chen-Hsin Chan1, Kun-Liang Lin1

  • 1Isotope Application Division, Institute of Nuclear Energy Research, Taoyuan City, Taiwan, ROC.

Nuclear Medicine and Biology
|December 23, 2018
PubMed
Abstract

Insights

A novel heterodimer peptide, NOTA-RGD-GE11, effectively targets both integrin αVβ3 and EGFR. This dual-targeting peptide demonstrates enhanced tumor uptake for improved cancer imaging applications.

Area of Science:

  • Biomedical Imaging
  • Radiochemistry
  • Molecular Oncology

Background:

  • Multiple peptide receptors, including integrin αVβ3 and EGFR, are frequently co-expressed in various cancers.
  • Targeting these receptors offers potential for specific cancer detection and therapy.

Purpose of the Study:

  • To design and characterize a novel heterodimer peptide, NOTA-c(RGDyK)-GE11 (NOTA-RGD-GE11), for dual-receptor targeting.
  • To evaluate the potential of NOTA-RGD-GE11 for dual integrin αVβ3 and EGFR-targeted tumor imaging.

Main Methods:

  • Synthesis and radiolabeling of NOTA-RGD-GE11 with Gallium-68 ([68Ga]).
  • Assessment of dual receptor binding affinity using antibody competition assays.
  • In vitro and in vivo evaluation of [68Ga]Ga-NOTA-RGD-GE11 characteristics, including tumor uptake and biodistribution in a NCI-H292 tumor model.

Main Results:

  • NOTA-RGD-GE11 exhibited binding affinities for both integrin αVβ3 and EGFR.
  • Dual receptor targeting was confirmed via blocking studies.
  • [68Ga]Ga-NOTA-RGD-GE11 demonstrated significantly higher tumor uptake compared to monomeric peptide analogs in biodistribution and PET/CT imaging.

Conclusions:

  • The heterodimer peptide NOTA-RGD-GE11 successfully targets both integrin αVβ3 and EGFR.
  • Enhanced tumor accumulation of [68Ga]Ga-NOTA-RGD-GE11 suggests its promise for dual-targeted cancer imaging.
  • Further investigation is warranted for clinical applications in dual integrin αVβ3 and EGFR-targeted tumor imaging.
Keywords:
EGFRGa-68Heterodimer peptideIntegrin α(V)β(3)PET imaging

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