Access the full text.
Sign up today, get DeepDyve free for 14 days.
Loading next page...
/lp/sage/synthesis-and-evaluation-of-optical-and-pet-glp-1-peptide-analogues-GJeZ4tIlI7
- Publisher
- SAGE
- Copyright
- Copyright © 2019 by SAGE Publications Inc, unless otherwise noted. Manuscript content on this site is licensed under Creative Commons Licenses
- ISSN
- 1536-0121
- eISSN
- 1536-0121
- DOI
- 10.2310/7290.2014.00057
- Publisher site
- See Article on Publisher Site
Abstract
A fluorescein-GLP-1 (7-37) analog was generated to determine GLP-1R distribution in various cell types of the pancreas in both strains of mice and receptor-specific uptake was confirmed by blocking with exendin-4. Biodistribution studies were carried out using 68Ga-labeled GLP-1 (7-37) peptides in CD1 and C57BL/6 mice. In addition, immunocompromised mice bearing GLP-1R-expressing insulinomas were evaluated by positron emission tomography (PET) imaging and ex vivo biodistribution studies. The optical GLP-1 probe strongly colocalized with immunofluorescence for insulin and glucagon, and more weakly with amylase (exocrine pancreas) and cytokeratin 19 (ductal cells), confirming its application for in situ GLP-1R imaging in various pancreatic cell types. Insulinomas were clearly visualized by in vivo PET. Reducing the peptide positive charge decreased renal retention as well as tumor uptake. Results demonstrate the application of the developed GLP-1 peptide analogues for in situ (optical) and in vivo (PET) imaging of GLP-1R expression.
Journal
Molecular Imaging – SAGE
Published: Jul 27, 2017