Triple-peptide receptor targeting in vitro allows detection of all tested gut and bronchial NETs.

Reubi, Jean Claude; Waser, Beatrice (2015). Triple-peptide receptor targeting in vitro allows detection of all tested gut and bronchial NETs. Journal of nuclear medicine, 56(4), pp. 613-615. Society of Nuclear Medicine 10.2967/jnumed.114.153189

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UNLABELLED A high proportion of gut and bronchial neuroendocrine tumors (NETs) overexpresses somatostatin receptors, especially the sst2 subtype. It has also recently been observed that incretin receptors, namely glucagonlike peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) receptors, can be overexpressed in gut and bronchial NETs. However, because not all tumors can express these receptors in sufficient amounts, in vivo imaging with a single radioligand may not always be successful. We therefore evaluated with in vitro methods whether a cocktail of radioligands targeting these 3 receptors would improve tumor labeling. METHODS In vitro receptor autoradiography was performed on 55 NETs, comparing in each successive section of tumor the binding with a single radioligand, either (125)I-Tyr(3)-octreotide, (125)I-GLP-1(7-36)amide, or (125)I-GIP(1-30), with the binding using a cocktail of all 3 radioligands, given concomitantly under identical experimental conditions. RESULTS Using the cocktail of radioligands, all tumors without exception showed moderate to very high binding, with a receptor density corresponding to 1,000-10,000 dpm/mg of tissue; conversely, single-ligand binding, although identifying most tumors as receptor-positive, failed to detect receptors or measured only a low density of receptors below 1,000 dpm/mg in a significant number of tumors. In addition, the cocktail of radioligands always provided a homogeneous labeling of the whole tumor, whereas single radioligands occasionally showed heterogeneous labeling. CONCLUSION The study suggests that the use of a cocktail of 3 radioligands binding to somatostatin receptors, GLP-1 receptors, and GIP receptors would allow detecting virtually all NETs and labeling them homogeneously in vivo, representing a significant improvement for imaging and therapy in NETs.

Item Type:

Journal Article (Original Article)


04 Faculty of Medicine > Service Sector > Institute of Pathology

UniBE Contributor:

Reubi-Kattenbusch, Jean-Claude and Waser, Beatrice


500 Science > 570 Life sciences; biology
600 Technology > 610 Medicine & health




Society of Nuclear Medicine




Doris Haefelin

Date Deposited:

13 Jul 2015 13:58

Last Modified:

17 Oct 2019 11:09

Publisher DOI:


PubMed ID:


Uncontrolled Keywords:

GLP-1 receptors; incretin receptors; multireceptor imaging; neuroendocrine tumors; somatostatin receptors




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