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Updated: Jan 22, 2026
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In situ Quantification of Pancreatic Beta-cell Mass in Mice
Published on: June 7, 2010
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GPR44 as a Target for Imaging Pancreatic Beta-Cell Mass
1Science for Life Laboratory, Department of Medicinal Chemistry, Uppsala University, Dag Hammarskjölds väg 14C, 3tr, SE-752 37, Uppsala, Sweden. olof.eriksson@ilk.uu.se.
Current Diabetes Reports
|June 29, 2019
Summary
New positron emission tomography (PET) imaging markers targeting GPR44 show promise for measuring beta-cell mass (BCM). These GPR44-targeting radioligands could enable non-invasive BCM assessment for metabolic disease diagnosis and treatment.
Area of Science:
- Endocrinology
- Nuclear Medicine
- Molecular Imaging
Background:
- Accurate, non-invasive quantitative markers for human beta-cell mass (BCM) are currently unavailable.
- Positron emission tomography (PET) imaging offers a potential solution for BCM measurement using beta-cell specific targets.
- GPR44 has been identified as a promising novel marker for beta cells.
Purpose of the Study:
- To review the development of GPR44 as a target for PET imaging of BCM.
- To summarize recent advancements in GPR44-targeting radioligands for BCM visualization.
Main Methods:
- Radiolabeling of small molecule binders targeting GPR44.
- In vitro and in vivo evaluation of radioligands in animal models.
- Assessment of binding affinity, specificity, and dose-dependency to beta cells.
Main Results:
- Several GPR44-targeting radioligands were developed and evaluated.
- Radioligands like 11C-AZ12204657 and 11C-MK-7246 demonstrated dose-dependent, GPR44-mediated binding to beta cells.
- Negligible uptake in the exocrine pancreas was observed, indicating target specificity.
Conclusions:
- GPR44 is a viable target for PET imaging of BCM.
- Further development and clinical testing of GPR44 radioligands are anticipated.
- GPR44 may serve as a valuable surrogate marker for human BCM assessment.
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