Radiolabelled GLP-1 receptor antagonist binds to GLP-1 receptor-expressing human tissues.

Waser, Beatrice; Reubi, Jean-Claude (2014). Radiolabelled GLP-1 receptor antagonist binds to GLP-1 receptor-expressing human tissues. European journal of nuclear medicine and molecular imaging, 41(6), pp. 1166-1171. Springer 10.1007/s00259-013-2684-4

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PURPOSE Radiolabelled glucagon-like peptide 1 (GLP-1) receptor agonists have recently been shown to successfully image benign insulinomas in patients. For the somatostatin receptor targeting of tumours, however, it was recently reported that antagonist tracers were superior to agonist tracers. The present study therefore evaluated various forms of the (125)iodinated-Bolton-Hunter (BH)-exendin(9-39) antagonist tracer for the in vitro visualization of GLP-1 receptor-expressing tissues in rats and humans and compared it with the agonist tracer (125)I-GLP-1(7-36)amide. METHODS Receptor autoradiography studies with (125)I-GLP-1(7-36)amide agonist or (125)I-BH-exendin(9-39) antagonist radioligands were performed in human and rat tissues. RESULTS The antagonist (125)I-BH-exendin(9-39) labelled at lysine 19 identifies all human and rat GLP-1 target tissues and GLP-1 receptor-expressing tumours. Binding is of high affinity and is comparable in all tested tissues in its binding properties with the agonist tracer (125)I-GLP-1(7-36)amide. For comparison, (125)I-BH-exendin(9-39) with the BH labelled at lysine 4 did identify the GLP-1 receptor in rat tissues but not in human tissues. CONCLUSION The GLP-1 receptor antagonist exendin(9-39) labelled with (125)I-BH at lysine 19 is an excellent GLP-1 radioligand that identifies human and rat GLP-1 receptors in normal and tumoural tissues. It may therefore be the molecular basis to develop suitable GLP-1 receptor antagonist radioligands for in vivo imaging of GLP-1 receptor-expressing tissues in patients.

Item Type:

Journal Article (Original Article)

Division/Institute:

04 Faculty of Medicine > Service Sector > Institute of Pathology

UniBE Contributor:

Waser, Beatrice and Reubi-Kattenbusch, Jean-Claude

Subjects:

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

ISSN:

1619-7070

Publisher:

Springer

Language:

English

Submitter:

Doris Haefelin

Date Deposited:

13 Apr 2015 11:27

Last Modified:

10 Oct 2019 14:28

Publisher DOI:

10.1007/s00259-013-2684-4

PubMed ID:

24519555

BORIS DOI:

10.7892/boris.66521

URI:

https://boris.unibe.ch/id/eprint/66521

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