Glucagon-like peptide-1 receptor overexpression in cancer and its impact on clinical applications

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 over-expressed in various human tumor types and therefore represent molecular targets for important clinical applications. In particular, virtua...

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Main Authors: Meike eKörner, Emanuel eChrist, Damian eWild, Jean Claude eReubi
Format: Article
Language:English
Published: Frontiers Media S.A. 2012-12-01
Series:Frontiers in Endocrinology
Subjects:
Online Access:http://journal.frontiersin.org/Journal/10.3389/fendo.2012.00158/full
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author Meike eKörner
Emanuel eChrist
Damian eWild
Jean Claude eReubi
author_facet Meike eKörner
Emanuel eChrist
Damian eWild
Jean Claude eReubi
author_sort Meike eKörner
collection DOAJ
description 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 over-expressed in various human tumor types and therefore represent molecular targets for important clinical applications. In particular, virtually all benign insulinomas highly over-express 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 monitore patients undergoing GLP-1 therapy carefully.
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spelling doaj.art-18abe4f965fb4feba84c90f6491ae8302022-12-22T02:02:44ZengFrontiers Media S.A.Frontiers in Endocrinology1664-23922012-12-01310.3389/fendo.2012.0015835115Glucagon-like peptide-1 receptor overexpression in cancer and its impact on clinical applicationsMeike eKörner0Emanuel eChrist1Damian eWild2Jean Claude eReubi3Institute of Pathology, University of BerneUniversity Hospital BerneUniversitätsspital BaselInstitute of Pathology, University of BernePeptide hormones of the glucagon-like peptide (GLP) family play an increasing clinical role, such as GLP-1 in diabetes therapy. Moreover, GLP receptors are over-expressed in various human tumor types and therefore represent molecular targets for important clinical applications. In particular, virtually all benign insulinomas highly over-express 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 monitore patients undergoing GLP-1 therapy carefully.http://journal.frontiersin.org/Journal/10.3389/fendo.2012.00158/fullInsulinomasomatostatin receptorsGlucagon-like peptide-1Glucagon-like petide-1 receptor111In-DOTA/DPTA-exendin-4.
spellingShingle Meike eKörner
Emanuel eChrist
Damian eWild
Jean Claude eReubi
Glucagon-like peptide-1 receptor overexpression in cancer and its impact on clinical applications
Frontiers in Endocrinology
Insulinoma
somatostatin receptors
Glucagon-like peptide-1
Glucagon-like petide-1 receptor
111In-DOTA/DPTA-exendin-4.
title Glucagon-like peptide-1 receptor overexpression in cancer and its impact on clinical applications
title_full Glucagon-like peptide-1 receptor overexpression in cancer and its impact on clinical applications
title_fullStr Glucagon-like peptide-1 receptor overexpression in cancer and its impact on clinical applications
title_full_unstemmed Glucagon-like peptide-1 receptor overexpression in cancer and its impact on clinical applications
title_short Glucagon-like peptide-1 receptor overexpression in cancer and its impact on clinical applications
title_sort glucagon like peptide 1 receptor overexpression in cancer and its impact on clinical applications
topic Insulinoma
somatostatin receptors
Glucagon-like peptide-1
Glucagon-like petide-1 receptor
111In-DOTA/DPTA-exendin-4.
url http://journal.frontiersin.org/Journal/10.3389/fendo.2012.00158/full
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