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GPR44 as a Target for Imaging Pancreatic Beta-Cell Mass
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Theranostics. Uppsala University, Science for Life Laboratory, SciLifeLab. Antaros Med AB, Molndal, Sweden.ORCID iD: 0000-0002-2515-8790
2019 (English)In: Current Diabetes Reports, ISSN 1534-4827, E-ISSN 1539-0829, Vol. 19, no 8, article id 49Article, review/survey (Refereed) Published
Abstract [en]

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. C-11-AZ12204657 and C-11-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. Summary 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.

Place, publisher, year, edition, pages
Springer, 2019. Vol. 19, no 8, article id 49
Keywords [en]
Beta-cell imaging, Islet imaging, Beta-cell mass, GPR44, PET, Diabetes
National Category
Endocrinology and Diabetes
Identifiers
URN: urn:nbn:se:uu:diva-390420DOI: 10.1007/s11892-019-1164-zISI: 000473164900004PubMedID: 31250117OAI: oai:DiVA.org:uu-390420DiVA, id: diva2:1342081
Available from: 2019-08-12 Created: 2019-08-12 Last updated: 2019-08-12Bibliographically approved

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