GLP-2 receptors in human disease: high expression in gastrointestinal stromal tumors and Crohn's disease.

Abstract

Peptide hormones of the glucagon-like peptide (GLP) family play an increasing clinical role, as reported for GLP-1 in diabetes therapy and insulinoma diagnostics. GLP-2, despite its known trophic and anti-inflammatory intestinal actions translated into preliminary clinical studies using the GLP-2 analogue teduglutide for treatment of short bowel syndrome and Crohn's disease, remains poorly characterized in terms of expression of its receptor in tissues of interest. Therefore, the GLP-2 receptor expression was assessed in 237 tumor and 148 non-neoplastic tissue samples with in vitro receptor autoradiography. A GLP-2 receptor expression was present in 68% of gastrointestinal stromal tumors (GIST). Furthermore, GLP-2 receptors were identified in the intestinal myenteric plexus, with significant up-regulation in active Crohn's disease. The GLP-2 receptors in GIST may be used for clinical applications like in vivo targeting with radiolabelled GLP-2 analogues for imaging and therapy. Moreover, the over-expressed GLP-2 receptor in the myenteric plexus may represent the morphological correlate of the clinical target of teduglutide in Crohn's disease.

• Authors: Meike Körner, Ruth Rehmann, Jean Claude Reubi
• Journal: Molecular and cellular endocrinology (Mol Cell Endocrinol) Vol. 364 Issue 1-2 Pg. 46-53 (Nov 25 2012) ISSN: 1872-8057 [Electronic] Ireland
• PMID: 22951144 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier Ireland Ltd. All rights reserved.

Chemical References

• GLP2R protein, human
• Glucagon-Like Peptide 2
• Glucagon-Like Peptide-2 Receptor
• Receptors, Glucagon

Topics

• Adult
• Aged
• Autoradiography
• Crohn Disease (genetics, metabolism, pathology)
• Female
• Gastrointestinal Neoplasms (genetics, metabolism, pathology)
• Gastrointestinal Stromal Tumors (genetics, metabolism, pathology)
• Gene Expression
• Glucagon-Like Peptide 2 (metabolism)
• Glucagon-Like Peptide-2 Receptor
• Humans
• Intestinal Mucosa (metabolism)
• Intestines (pathology)
• Middle Aged
• Myenteric Plexus (metabolism, pathology)
• Receptors, Glucagon (genetics, metabolism)
• Up-Regulation