GPR44 as a Target for Imaging Pancreatic Beta-Cell Mass
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Updated: Jan 22, 2026

In situ Quantification of Pancreatic Beta-cell Mass in Mice
Published on: June 7, 2010
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.
Purpose Of Review:
Quantitative markers for beta-cell mass (BCM) in human pancreas are currently lacking. Medical imaging using positron emission tomography (PET) markers for beta-cell restricted targets may provide an accurate and non-invasive measurement of BCM, to assist diagnosis and treatment of metabolic disease. GPR44 was recently discovered as a putative marker for beta cells and this review summarizes the developments so far.
Recent Findings:
Several small molecule binders targeting GPR44 have been radiolabeled for PET imaging and evaluated in vitro and in small and large animal models. 11C-AZ12204657 and 11C-MK-7246 displayed a dose-dependent and GPR44-mediated binding to beta cells both in vitro and in vivo, with negligible uptake in exocrine pancreas. GPR44 represents an attractive target for visualization of BCM. Further progress in radioligand development including clinical testing is expected to clarify the role of GPR44 as a surrogate marker for BCM in humans.
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