Bibliographic Details
| Title: |
PET Imaging of GPR44 by Antagonist [11C]MK-7246 in Pigs |
| Authors: |
Pierre Cheung, Bo Zhang, Emmi Puuvuori, Sergio Estrada, Mohammad A. Amin, Sofie Ye, Olle Korsgren, Luke R. Odell, Jonas Eriksson, Olof Eriksson |
| Source: |
Biomedicines, Vol 9, Iss 4, p 434 (2021) |
| Publisher Information: |
MDPI AG, 2021. |
| Publication Year: |
2021 |
| Collection: |
LCC:Biology (General) |
| Subject Terms: |
pancreas imaging, diabetes, biomarker, PET, PTGDR2, Biology (General), QH301-705.5 |
| More Details: |
A validated imaging marker for beta-cell mass would improve understanding of diabetes etiology and enable new strategies in therapy development. We previously identified the membrane-spanning protein GPR44 as highly expressed and specific to the beta cells of the pancreas. The selective GPR44 antagonist MK-7246 was radiolabeled with carbon-11 and the resulting positron-emission tomography (PET) tracer [11C]MK-7246 was evaluated in a pig model and in vitro cell lines. The [11C]MK-7246 compound demonstrated mainly hepatobiliary excretion with a clearly defined pancreas, no spillover from adjacent tissues, and pancreatic binding similar in magnitude to the previously evaluated GPR44 radioligand [11C]AZ12204657. The binding could be blocked by preadministration of nonradioactive MK-7246, indicating a receptor-binding mechanism. [11C]MK-7246 showed strong potential as a PET ligand candidate for visualization of beta-cell mass (BCM) and clinical translation of this methodology is ongoing. |
| Document Type: |
article |
| File Description: |
electronic resource |
| Language: |
English |
| ISSN: |
2227-9059 |
| Relation: |
https://www.mdpi.com/2227-9059/9/4/434; https://doaj.org/toc/2227-9059 |
| DOI: |
10.3390/biomedicines9040434 |
| Access URL: |
https://doaj.org/article/a98421e8f5e64dde94a575e5283caa46 |
| Accession Number: |
edsdoj.98421e8f5e64dde94a575e5283caa46 |
| Database: |
Directory of Open Access Journals |
