GPR44 As a Target for Imaging Pancreatic Beta-Cell Mass

Overview

Journal Curr Diab Rep

Publisher Current Science

Specialty Endocrinology

Date 2019 Jun 29

PMID 31250117

Citations 9

Authors

Olof Eriksson

Affiliations

Soon will be listed here.

Abstract

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-AZ12204657 and C-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.

Citing Articles

One-Step Automatic Radiosynthesis and Evaluation of [F]TM-30089 as GPR44 Radiotracer.

Peng J, Tang W, Rawson J, Miao L, Gonzalez N, Yin R Pharmaceuticals (Basel). 2023; 16(10).

PMID: 37895951 PMC: 10610095. DOI: 10.3390/ph16101480.

Indole-Based and Cyclopentenylindole-Based Analogues Containing Fluorine Group as Potential F-Labeled Positron Emission Tomography (PET) G-Protein Coupled Receptor 44 (GPR44) Tracers.

Yin R, Huang K, Huang L, Ji M, Zhao H, Li K Pharmaceuticals (Basel). 2023; 16(9).

PMID: 37765011 PMC: 10534865. DOI: 10.3390/ph16091203.

[F]MK-7246 for Positron Emission Tomography Imaging of the Beta-Cell Surface Marker GPR44.

Cheung P, Amin M, Zhang B, Lechi F, Korsgren O, Eriksson J Pharmaceutics. 2023; 15(2).

PMID: 36839820 PMC: 9962486. DOI: 10.3390/pharmaceutics15020499.

Identification and Validation of a New Peptide Targeting Pancreatic Beta Cells.

Wang Q, Zheng L, Wu K, Zhang B Molecules. 2022; 27(7).

PMID: 35408679 PMC: 9000318. DOI: 10.3390/molecules27072286.

Imaging β-Cell Function Using a Zinc-Responsive MRI Contrast Agent May Identify First Responder Islets.

Thapa B, Suh E, Parrott D, Khalighinejad P, Sharma G, Chirayil S Front Endocrinol (Lausanne). 2022; 12:809867.

PMID: 35173681 PMC: 8842654. DOI: 10.3389/fendo.2021.809867.

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