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Low kidney uptake of GLP-1R-targeting, beta cell-specific PET tracer, 18F-labeled [Nle14,Lys40]exendin-4 analog, shows promise for clinical imaging

Overview of attention for article published in EJNMMI Research, December 2016
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Title
Low kidney uptake of GLP-1R-targeting, beta cell-specific PET tracer, 18F-labeled [Nle14,Lys40]exendin-4 analog, shows promise for clinical imaging
Published in
EJNMMI Research, December 2016
DOI 10.1186/s13550-016-0243-2
Pubmed ID
Authors

Kirsi Mikkola, Cheng-Bin Yim, Paula Lehtiniemi, Saila Kauhanen, Miikka Tarkia, Tuula Tolvanen, Pirjo Nuutila, Olof Solin

Abstract

Several radiometal-labeled, exendin-based tracers that target glucagon-like peptide-1 receptors (GLP-1R) have been intensively explored for β cell imaging. The main obstacle has been the high uptake of tracer in the kidneys. This study aimed to develop a novel GLP1-R-specific tracer, with fluorine-18 attached to exendin-4, to label β cells for clinical imaging with PET (positron emission tomography). We hypothesized that this tracer would undergo reduced kidney uptake. (18)F-labeled [Nle(14),Lys(40)]exendin-4 analog ([(18)F]exendin-4) was produced via Cu-catalyzed click chemistry. The biodistribution of [(18)F]exendin-4 was assessed with ex vivo organ γ-counting and in vivo PET imaging. We also tested the in vivo stability of the radiotracer. The localization of (18)F radioactivity in rat and human pancreatic tissue sections was investigated with autoradiography. Receptor specificity was assessed with unlabeled exendin-3. Islet labeling was confirmed with immunohistochemistry. The doses of radiation in humans were estimated based on biodistribution results in rats. [(18)F]exendin-4 was synthesized with high yield and high specific activity. Results showed specific, sustained [(18)F]exendin-4 uptake in pancreatic islets. In contrast to previous studies that tested radiometal-labeled exendin-based tracers, we observed rapid renal clearance of [(18)F]exendin-4. [(18)F]exendin-4 showed promise as a tracer for clinical imaging of pancreatic β cells, due to its high specific uptake in native β cells and its concomitant low kidney radioactivity uptake.

Twitter Demographics

The data shown below were collected from the profile of 1 tweeter who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 14 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 14 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 3 21%
Student > Doctoral Student 2 14%
Student > Master 2 14%
Researcher 2 14%
Professor 1 7%
Other 3 21%
Unknown 1 7%
Readers by discipline Count As %
Chemistry 3 21%
Biochemistry, Genetics and Molecular Biology 2 14%
Pharmacology, Toxicology and Pharmaceutical Science 2 14%
Medicine and Dentistry 2 14%
Agricultural and Biological Sciences 2 14%
Other 1 7%
Unknown 2 14%

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 03 January 2017.
All research outputs
#4,790,874
of 8,849,667 outputs
Outputs from EJNMMI Research
#65
of 192 outputs
Outputs of similar age
#167,586
of 301,696 outputs
Outputs of similar age from EJNMMI Research
#14
of 31 outputs
Altmetric has tracked 8,849,667 research outputs across all sources so far. This one is in the 27th percentile – i.e., 27% of other outputs scored the same or lower than it.
So far Altmetric has tracked 192 research outputs from this source. They receive a mean Attention Score of 1.7. This one has gotten more attention than average, scoring higher than 53% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 301,696 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 34th percentile – i.e., 34% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 31 others from the same source and published within six weeks on either side of this one. This one is in the 41st percentile – i.e., 41% of its contemporaries scored the same or lower than it.