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Article

Sigma-1 Receptor Positron Emission Tomography: A New Molecular Imaging Approach Using (S)-(−)-[18F]Fluspidine in Glioblastoma

1
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Institute of Radiopharmaceutical Cancer Research, Department of Neuroradiopharmaceuticals, Research site Leipzig, 04318 Leipzig, Germany
2
PET Imaging Center, University Hospital of North Norway (UNN), 9009 Tromsø, Norway
3
Nuclear Medicine and Radiation Biology Research Group, The Arctic University of Norway, 9009 Tromsø, Norway
4
Department of Neurosurgery, Technische Universität Dresden (TUD), University Hospital Carl Gustav Carus, 01307 Dresden, Germany
5
Department of Nuclear Medicine, University Hospital Leipzig, 04318 Leipzig, Germany
6
Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, 48149 Münster, Germany
*
Author to whom correspondence should be addressed.
Academic Editors: Anne Roivainen and Xiang-Guo Li
Molecules 2020, 25(9), 2170; https://doi.org/10.3390/molecules25092170
Received: 13 April 2020 / Revised: 30 April 2020 / Accepted: 2 May 2020 / Published: 6 May 2020
(This article belongs to the Special Issue Radiopharmaceuticals for PET Imaging - Issue A)
Glioblastoma multiforme (GBM) is the most devastating primary brain tumour characterised by infiltrative growth and resistance to therapies. According to recent research, the sigma-1 receptor (sig1R), an endoplasmic reticulum chaperone protein, is involved in signaling pathways assumed to control the proliferation of cancer cells and thus could serve as candidate for molecular characterisation of GBM. To test this hypothesis, we used the clinically applied sig1R-ligand (S)-(−)-[18F]fluspidine in imaging studies in an orthotopic mouse model of GBM (U87-MG) as well as in human GBM tissue. A tumour-specific overexpression of sig1R in the U87-MG model was revealed in vitro by autoradiography. The binding parameters demonstrated target-selective binding according to identical KD values in the tumour area and the contralateral side, but a higher density of sig1R in the tumour. Different kinetic profiles were observed in both areas, with a slower washout in the tumour tissue compared to the contralateral side. The translational relevance of sig1R imaging in oncology is reflected by the autoradiographic detection of tumour-specific expression of sig1R in samples obtained from patients with glioblastoma. Thus, the herein presented data support further research on sig1R in neuro-oncology. View Full-Text
Keywords: sigma-1 receptor availability; orthotopic xenograft of glioblastoma in mouse; small animal Positron Emission Tomography/Magnetic Resonance Imaging (PET/MRI); (S)-(−)-[18F]fluspidine; imaging-based biomarker sigma-1 receptor availability; orthotopic xenograft of glioblastoma in mouse; small animal Positron Emission Tomography/Magnetic Resonance Imaging (PET/MRI); (S)-(−)-[18F]fluspidine; imaging-based biomarker
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MDPI and ACS Style

Toussaint, M.; Deuther-Conrad, W.; Kranz, M.; Fischer, S.; Ludwig, F.-A.; Juratli, T.A.; Patt, M.; Wünsch, B.; Schackert, G.; Sabri, O.; Brust, P. Sigma-1 Receptor Positron Emission Tomography: A New Molecular Imaging Approach Using (S)-(−)-[18F]Fluspidine in Glioblastoma. Molecules 2020, 25, 2170. https://doi.org/10.3390/molecules25092170

AMA Style

Toussaint M, Deuther-Conrad W, Kranz M, Fischer S, Ludwig F-A, Juratli TA, Patt M, Wünsch B, Schackert G, Sabri O, Brust P. Sigma-1 Receptor Positron Emission Tomography: A New Molecular Imaging Approach Using (S)-(−)-[18F]Fluspidine in Glioblastoma. Molecules. 2020; 25(9):2170. https://doi.org/10.3390/molecules25092170

Chicago/Turabian Style

Toussaint, Magali, Winnie Deuther-Conrad, Mathias Kranz, Steffen Fischer, Friedrich-Alexander Ludwig, Tareq A. Juratli, Marianne Patt, Bernhard Wünsch, Gabriele Schackert, Osama Sabri, and Peter Brust. 2020. "Sigma-1 Receptor Positron Emission Tomography: A New Molecular Imaging Approach Using (S)-(−)-[18F]Fluspidine in Glioblastoma" Molecules 25, no. 9: 2170. https://doi.org/10.3390/molecules25092170

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