Radiolabelled GLP-1 receptor antagonist binds to GLP-1 receptor-expressing human tissues
European Journal of Nuclear Medicine and Molecular Imaging, ISSN: 1619-7089, Vol: 41, Issue: 6, Page: 1166-1171
2014
- 24Citations
- 31Captures
Metric Options: Counts1 Year3 YearSelecting the 1-year or 3-year option will change the metrics count to percentiles, illustrating how an article or review compares to other articles or reviews within the selected time period in the same journal. Selecting the 1-year option compares the metrics against other articles/reviews that were also published in the same calendar year. Selecting the 3-year option compares the metrics against other articles/reviews that were also published in the same calendar year plus the two years prior.
Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
Citation Benchmarking is provided by Scopus and SciVal and is different from the metrics context provided by PlumX Metrics.
Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
Citation Benchmarking is provided by Scopus and SciVal and is different from the metrics context provided by PlumX Metrics.
Metrics Details
- Citations24
- Citation Indexes24
- 24
- CrossRef10
- Captures31
- Readers31
- 31
Article Description
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 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 I-GLP-1(7-36)amide. Methods: Receptor autoradiography studies with I-GLP-1(7-36)amide agonist or I-BH-exendin(9-39) antagonist radioligands were performed in human and rat tissues. Results: The antagonist 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 I-GLP-1(7-36)amide. For comparison, 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 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. © 2014 Springer-Verlag Berlin Heidelberg.
Bibliographic Details
http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84900833578&origin=inward; http://dx.doi.org/10.1007/s00259-013-2684-4; http://www.ncbi.nlm.nih.gov/pubmed/24519555; http://link.springer.com/10.1007/s00259-013-2684-4; https://dx.doi.org/10.1007/s00259-013-2684-4; https://link.springer.com/article/10.1007/s00259-013-2684-4
Springer Science and Business Media LLC
Provide Feedback
Have ideas for a new metric? Would you like to see something else here?Let us know