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Updated: Jun 24, 2026
Preparing a 68Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis
Published on: January 7, 2019
New targeted probes for radioimaging of angiogenesis
T H Stollman1, T J M Ruers, W J G Oyen
1Department of Surgery, Radboud University Nijmegen Medical Center, P.O. Box 9101, 6500 HB Nijmegen, The Netherlands. T.Stollman@chir.umcn.nl
Abstract:
Angiogenesis, the formation of new blood vessels, is a multi-step process regulated by pro- and anti-angiogenic factors. In order to grow and metastasize, tumors need a constant supply of oxygen and nutrients. For their growth beyond the size of 1-2 mm tumors are dependent on angiogenesis. Recently, various new anti-cancer agents (e.g. bevacizumab, sorafenib and sunitinib) have become available that specifically inhibit angiogenesis in tumors. To evaluate the effects of these new anti-angiogenic agents it would be of interest to scintigraphically image the process of angiogenesis in tumors. Several markers have been described that are preferentially expressed on newly formed blood vessels in tumors (alpha(v)beta(3) integrin, vascular endothelial growth factor and its receptor, prostate-specific membrane antigen) and in the extracellular matrix surrounding newly formed blood vessels (extra-domain B of fibronectin, Tenascin-C, matrix metalloproteinases, Robo-4). Several ligands targeting these markers have been tested as a radiotracer for imaging angiogenesis in tumors. The potential of some of these tracers such as radiolabeled cyclic RGD peptides and radiolabeled anti-PSMA antibodies has already been tested cancer patients, while for markers such as Robo-4 the ligand has not yet been identified. Here the preclinical and clinical studies with these new tracers to image angiogenesis in tumors are reviewed.
Insights
New radiotracers can image tumor angiogenesis, the process of new blood vessel formation essential for tumor growth. This review covers preclinical and clinical studies of tracers targeting tumor angiogenesis markers.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Tumor growth and metastasis depend on angiogenesis, the formation of new blood vessels.
- New anti-cancer agents target angiogenesis, necessitating methods to evaluate their efficacy.
- Several molecular markers on tumor vasculature and the extracellular matrix are targets for imaging agents.
Purpose of the Study:
- To review preclinical and clinical studies of radiotracers for imaging tumor angiogenesis.
- To discuss the potential of various targeted radiotracers for evaluating anti-angiogenic therapies.
Main Methods:
- Review of published preclinical and clinical studies on radiotracers for tumor angiogenesis imaging.
- Identification of markers expressed on tumor neovasculature and extracellular matrix.
- Evaluation of ligands targeting these markers as potential radiotracers.
Main Results:
- Various markers like alpha(v)beta(3) integrin, VEGF, PSMA, and Robo-4 are associated with tumor angiogenesis.
- Radiolabeled cyclic RGD peptides and anti-PSMA antibodies have shown potential in preclinical and clinical studies.
- Ligands for some markers, such as Robo-4, are still under investigation.
Conclusions:
- Radiotracers targeting specific angiogenesis markers offer a promising approach for scintigraphic imaging of tumor neovasculature.
- These imaging techniques are crucial for evaluating the effectiveness of novel anti-angiogenic cancer therapies.
- Further development of targeted radiotracers is needed for comprehensive imaging of tumor angiogenesis.
