Evaluation of an [18F]AlF-NOTA Analog of Exendin-4 for Imaging of GLP-1 Receptor in Insulinoma
Open Access
- 1 January 2012
- journal article
- Published by Ivyspring International Publisher in Theranostics
- Vol. 2 (10), 999-1009
- https://doi.org/10.7150/thno.5276
Abstract
Introduction: The GLP-1 receptor plays an important role in glucose homeostasis and thus is a very important target for diabetes therapy. The receptor is also overexpressed in insulinoma, a tumor of pancreatic beta-cells. We previously evaluated two fluorine-18-labeled analogs of exendin-4 prepared by conjugation with [18F]FBEM (N-[2-(4-[18F]fluorobenzamide)ethyl]maleimide). Both compounds demonstrated good tumor uptake, but the synthesis of the radiotracers was time consuming. To overcome this challenge, we developed a NOTA analog and performed radiolabeling using aluminum [18F]fluoride complexation.Keywords
This publication has 26 references indexed in Scilit:
- A Novel Method of 18F Radiolabeling for PETJournal of Nuclear Medicine, 2009
- 18F, 64Cu, and 68Ga Labeled RGD-Bombesin Heterodimeric Peptides for PET Imaging of Breast CancerBioconjugate Chemistry, 2009
- Reducing Renal Uptake of Radiolabeled Peptides Using Albumin FragmentsJournal of Nuclear Medicine, 2008
- Expression of the GLP-1 Receptor in Mouse, Rat, and Human PancreasJournal of Histochemistry & Cytochemistry, 2008
- Cardioprotective and Vasodilatory Actions of Glucagon-Like Peptide 1 Receptor Are Mediated Through Both Glucagon-Like Peptide 1 Receptor–Dependent and –Independent PathwaysCirculation, 2008
- Glucagon-like peptide-1, glucose homeostasis and diabetesTrends in Molecular Medicine, 2008
- In Vivo Evaluation and Small-Animal PET/CT of a Prostate Cancer Mouse Model Using 64Cu Bombesin Analogs: Side-by-Side Comparison of the CB-TE2A and DOTA Chelation SystemsJournal of Nuclear Medicine, 2007
- [Lys40(Ahx-DTPA-111In)NH2]exendin-4, a very promising ligand for glucagon-like peptide-1 (GLP-1) receptor targeting.2006
- Concomitant expression of several peptide receptors in neuroendocrine tumours: molecular basis for in vivo multireceptor tumour targetingEuropean Journal of Nuclear Medicine and Molecular Imaging, 2003
- Imaging and localization of pancreatic insulinomasClinical Imaging, 2001