Toward molecular imaging of the free fatty acid receptor 1

Ewa Hellström‐Lindahl1, Ola Åberg1, Cecilia Ericsson2, Gavin O’Mahony2, Peter Johnström3, Stanko Skrtic2,4, Olof Eriksson1
1Division of Molecular Imaging, Department of Medicinal Chemistry, Uppsala University, Uppsala, Sweden
2AstraZeneca R&D, Mölndal, Sweden
3Personalised Healthcare and Biomarkers, AstraZeneca PET Science Centre, Karolinska Institutet, Karolinska University Hospital, Stockholm, Sweden
4Institute of Medicine, Sahlgrenska Academy, University of Gothenburg, Gothenburg, Sweden

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Negoro N, Sasaki S, Mikami S et al (2010) Discovery of TAK-875: a potent, selective, and orally bioavailable GPR40 agonist. ACS Med Chem Lett 1:290–294

Itoh Y, Kawamata Y, Harada M et al (2003) Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature 422:173–176

Hu H, He LY, Gong Z et al (2009) A novel class of antagonists for the FFAs receptor GPR40. Biochem Biophys Res Commun 390:557–563

Hara T, Hirasawa A, Sun Q et al (2009) Flow cytometry-based binding assay for GPR40 (FFAR1; free fatty acid receptor 1). Mol Pharmacol 75:85–91

Ren XM, Cao LY, Zhang J et al (2016) Investigation of the binding interaction of fatty acids with human G protein-coupled receptor 40 using a site-specific fluorescence probe by flow cytometry. Biochemistry 55:1989–1996

Bertrand R, Wolf A, Ivashchenko Y et al (2016) Synthesis and characterization of a promising novel FFAR1/GPR40 targeting fluorescent probe for β-cell imaging. ACS Chem Biol 11:1745–1754

Bertrand R, Hamp I, Brönstrup M et al (2016) Synthesis of GPR40 targeting 3H- and 18F-probes towards selective beta cell imaging. J Label Comp Radiopharm. doi: 10.1002/jlcr.3412

Eriksson O, Laughlin M, Brom M et al (2016) In vivo imaging of beta cells with radiotracers: state of the art, prospects and recommendations for development and use. Diabetologia 59:1340–1349

Flodgren E, Olde B, Meidute-Abaraviciene S, Winzell MS, Ahrén B, Salehi A (2007) GPR40 is expressed in glucagon producing cells and affects glucagon secretion. Biochem Biophys Res Com 354:240–245

Yashiro H, Tsujihata Y, Takeuchi K, Hazama M, Johnson PR, Rorsman P (2012) The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets. J Pharmacol Exp Ther 340:483–489

Doi H (2015) Pd-mediated rapid cross-couplings using [(11) C]methyl iodide: groundbreaking labeling methods in (11) C radiochemistry. J Label Comp Radiopharm 58:73–85

Pretze M, Grosse-Gehling P, Mamat C (2011) Cross-coupling reactions as valuable tool for the preparation of PET radiotracers. Molecules 16:1129–1165

Andersen VL, Herth MM, Lehel S, Knudsen GM, Kristensen JL (2013) Palladium-mediated conversion of para-aminoarylboronic esters into para-aminoaryl-11C-methanes. Tetrahedron Lett 54:213–216

Andersson Y, Aiping C, Långström B (1995) Palladium-promoted coupling reactions of [11C]methyl iodide with organotin and organoboron compounds. Acta Chem Scand 49:683–688