Abstract
Peptide hormones of the glucagon-like peptide (GLP) family play an increasing clinical role, such as GLP-1 in diabetes therapy. Moreover, GLP receptors are overexpressed in various human tumor types and therefore represent molecular targets for important clinical applications. In particular, virtually all benign insulinomas highly overexpress GLP-1 receptors (GLP-1R). Targeting GLP-1R with the stable GLP-1 analogs 111In-DOTA/DPTA-exendin-4 offers a new approach to successfully localize these small tumors. This non-invasive technique has the potential to replace the invasive localization of insulinomas by selective arterial stimulation and venous sampling. Malignant insulinomas, in contrast to their benign counterparts, express GLP-1R in only one-third of the cases, while they more often express the somatostatin type 2 receptors. Importantly, one of the two receptors appears to be always expressed in malignant insulinomas. The GLP-1R overexpression in selected cancers is worth to be kept in mind with regard to the increasing use of GLP-1 analogs for diabetes therapy. While the functional role of GLP-1R in neoplasia is not known yet, it may be safe to monitor patients undergoing GLP-1 therapy carefully.
Highlights
G protein-coupled peptide hormone receptors play an increasing role as tumor targets in cancer medicine (Reubi, 2003)
This review summarizes the knowledge on the in vitro and in vivo basis of glucagon-like peptide (GLP)-1 receptor targeting of tumors accumulated in the last decade
A more extensive study with data from 10 patients with malignant insulinoma showed that somatostatin receptors type 2 were expressed in seven patients, whereas glucagon-like peptide 1 (GLP-1) receptors (GLP-1R) were present in four patients, and both receptors in only one patient (Wild et al, 2011)
Summary
G protein-coupled peptide hormone receptors play an increasing role as tumor targets in cancer medicine (Reubi, 2003). This evaluation included the characterization of human tumors and normal tissues for their GLP-1R expression, since an important prerequisite for a successful peptide receptor www.frontiersin.org No other peptide receptor has been found to exhibit such high expression levels in this tumor type (Reubi and Waser, 2003).
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