Abstract
We report a single-molecule radiotracer that can be labeled independently with 18 F-fluoride or radiometals (64 Cu, 177 Lu) in a single step. A prostate-specific membrane antigen (PSMA)-targeting ligand, armed with both an organotrifluoroborate and a metal-chelator (DOTA), was designed to optionally afford 18 F-, 64 Cu- or 177 Lu-labeled products that were injected into mice bearing prostate cancer (LNCaP) xenografts. PET/CT images and ex vivo biodistribution data show high, specific tumor uptake irrespective of which radionuclide is used, thereby demonstrating a new approach to combining, in a single molecule, 18 F-labeling capabilities for PET imaging with radiometalation for potential imaging and therapeutic applications.
Keywords:
18F labeling; peptides; radiotracers; theranostics.
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antigens, Surface / chemistry
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Cell Line, Tumor
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Copper Radioisotopes / chemistry
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Fluorine Radioisotopes / chemistry
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Glutamate Carboxypeptidase II / chemistry
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Heterocyclic Compounds, 1-Ring / chemistry
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Humans
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Ligands
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Lutetium / chemistry
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Male
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Mice
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Positron Emission Tomography Computed Tomography
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Precision Medicine*
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Prostatic Neoplasms / diagnostic imaging
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Prostatic Neoplasms / pathology
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Radioisotopes / chemistry
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Radiopharmaceuticals / chemistry*
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Radiopharmaceuticals / metabolism
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Tissue Distribution
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Transplantation, Heterologous
Substances
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Antigens, Surface
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Copper Radioisotopes
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Copper-64
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Fluorine Radioisotopes
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Heterocyclic Compounds, 1-Ring
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Ligands
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Radioisotopes
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Radiopharmaceuticals
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1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
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Lutetium
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Lutetium-177
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FOLH1 protein, human
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Glutamate Carboxypeptidase II
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Fluorine-18