Radiolabelled peptides for oncological diagnosis

Eur J Nucl Med Mol Imaging. 2012 Feb;39 Suppl 1(Suppl 1):S78-92. doi: 10.1007/s00259-011-2014-7.


Radiolabelled receptor-binding peptides targeting receptors (over)expressed on tumour cells are widely under investigation for tumour diagnosis and therapy. The concept of using radiolabelled receptor-binding peptides to target receptor-expressing tissues in vivo has stimulated a large body of research in nuclear medicine. The (111)In-labelled somatostatin analogue octreotide (OctreoScan) is the most successful radiopeptide for tumour imaging, and was the first to be approved for diagnostic use. Based on the success of these studies, other receptor-targeting peptides such as cholecystokinin/gastrin analogues, glucagon-like peptide-1, bombesin (BN), chemokine receptor CXCR4 targeting peptides, and RGD peptides are currently under development or undergoing clinical trials. In this review, we discuss some of these peptides and their analogues, with regard to their potential for radionuclide imaging of tumours.

Publication types

  • Review

MeSH terms

  • Animals
  • Bombesin
  • Cholecystokinin
  • Glucagon-Like Peptide 1
  • Glucagon-Like Peptide-1 Receptor
  • Humans
  • Ligands
  • Neoplasms / diagnostic imaging*
  • Neoplasms / metabolism
  • Octreotide / analogs & derivatives
  • Pentetic Acid / analogs & derivatives
  • Peptides*
  • Radionuclide Imaging
  • Radiopharmaceuticals*
  • Receptor, Cholecystokinin B / metabolism
  • Receptors, Bombesin / metabolism
  • Receptors, CXCR4 / metabolism
  • Receptors, Cholecystokinin / metabolism
  • Receptors, Glucagon / metabolism


  • CXCR4 protein, human
  • GLP1R protein, human
  • Glucagon-Like Peptide-1 Receptor
  • Ligands
  • Peptides
  • Radiopharmaceuticals
  • Receptor, Cholecystokinin B
  • Receptors, Bombesin
  • Receptors, CXCR4
  • Receptors, Cholecystokinin
  • Receptors, Glucagon
  • SDZ 215-811
  • Pentetic Acid
  • Glucagon-Like Peptide 1
  • Cholecystokinin
  • Bombesin
  • Octreotide