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 journalArticlepeer-review

3 Scopus citations


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 111In. In vitro, 111In-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 ECRF24 cells was reduced in the presence of excess native Anginex. However, ex vivo biodistribution profiles showed little tumor uptake of 111In-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 noninvasive imaging of tumor angiogenesis using this peptide.

Original languageEnglish (US)
Pages (from-to)5945-5954
Number of pages10
JournalAnticancer Research
Issue number11
StatePublished - Nov 2015


  • Anginex
  • Cancer
  • Galectin-1
  • Indium-111
  • Tumor angiogenesis


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