Evaluation of 111In-labeled Anginex as Potential SPECT Tracer for Imaging of Tumor Angiogenesis

Tiemen R Van Mourik, Tilman Läppchen, Raffaella Rossin, Judy R Van Beijnum, John R Macdonald, Kevin H Mayo, Arjan W Griffioen, Klaas Nicolay, Holger Grüll

Research output: Contribution to journalArticleAcademicpeer-review


Angiogenesis is a prerequisite for solid tumors to grow and metastasize, providing oxygen and nutrients to the tumor site. The protein galectin-1 has been identified to be overexpressed on tumor vasculature and represents an interesting target for anti-angiogenic therapy, as well as in molecular imaging. Therefore, the galectin-1-binding peptide Anginex was modified for radiolabeling using (111)In. In vitro, (111)In-Ax showed significantly more binding to galectin-1-positive EC-RF24 and MDA-MB-231-LITG cells than to galectin-1-negative LS174T cells and association with EC-RF24 cells was reduced in the presence of excess native Anginex. However, ex vivo biodistribution profiles showed little tumor uptake of (111)In-Ax and extensive accumulation in non-target organs. Although this study shows the ease of modification of the therapeutic peptide Anginex and favorable characteristics in vitro, in vivo assessment of the tracer revealed negligible tumor targeting. Hence, the strategy we employed lends little support for successful non-invasive imaging of tumor angiogenesis using this peptide.

Original languageEnglish
Pages (from-to)5945-54
Number of pages10
JournalAnticancer research
Issue number11
Publication statusPublished - Nov 2015


  • Animals
  • Breast Neoplasms/diagnostic imaging
  • Colonic Neoplasms/diagnostic imaging
  • Female
  • Flow Cytometry
  • Galectin 1/metabolism
  • Humans
  • Image Processing, Computer-Assisted
  • Indium Radioisotopes/pharmacokinetics
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Neovascularization, Pathologic/diagnostic imaging
  • Peptides/pharmacokinetics
  • Radioactive Tracers
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon/methods
  • Tumor Cells, Cultured
  • Xenograft Model Antitumor Assays

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