This study reports the radiosynthesis of a new fluorine-18 glycosylated 'click' cyanoquinoline [(18) F]5 for positron emission tomography imaging of epidermal growth factor receptor (EGFR). The tracer was obtained in 47.7 ± 7.5% (n = 3) decay-corrected radiochemical yield from 2-[(18) F]fluoro-2-deoxy-β-d-glucopyranosyl azide, and the overall nondecay-corrected radiochemical yield from aqueous fluoride was 8.6 ± 2.3% (n = 3). An in vitro preliminary cellular uptake study showed selectivity of the tracer for EGFR-positive A431 cell lines versus EGFR-negative MCF-7 cell lines. [(18) F]5 tracer uptake in A431 cells was significantly reduced by addition of the cold isotope analogue compound 5.
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http://dx.doi.org/10.1002/jlcr.3170 | DOI Listing |
Cancers (Basel)
July 2024
Department of Nuclear Medicine, Molecular Imaging and Radiochemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg (FAU), 91054 Erlangen, Germany.
About 75% of breast tumors show an overexpression of the estradiol receptor (ER), making it a valuable target for tumor diagnosis and therapy. To date, 16-[F]fluoroestradiol (FES) is the only FDA-approved imaging probe for the positron emission tomography (PET) imaging of ER-positive (ER breast cancer. However, FES has the drawback of a high retention in the liver.
View Article and Find Full Text PDFPharmaceuticals (Basel)
November 2022
Université de Lorraine, CNRS, L2CM, F-54000 Nancy, France.
Considering the individual characteristics of positron emission tomography (PET) and optical imaging (OI) in terms of sensitivity, spatial resolution, and tissue penetration, the development of dual imaging agents for bimodal PET/OI imaging is a growing field. A current major breakthrough in this field is the design of monomolecular agent displaying both a radioisotope for PET and a fluorescent dye for OI. We took advantage of the multifunctionalities allowed by a clickable -glycosyl scaffold to gather the different elements.
View Article and Find Full Text PDFJ Nucl Med
December 2020
Friedrich-Alexander University Erlangen-Nürnberg (FAU), Department of Nuclear Medicine, Molecular Imaging and Radiochemistry, Translational Research Center, Erlangen, Germany
ACS Chem Neurosci
May 2020
Department of Clinical Neuroscience, Center for Psychiatry Research, Karolinska Institutet and Stockholm County Council, 17176 Stockholm, Sweden.
Gangliosides are biologically important glycolipids widely distributed in vertebrate cells. An important member of the ganglioside family is the monosialylganglioside GM1, which has been suggested as a potential therapeutic for Parkinson's disease. In the current study, a late-stage radiofluorination protocol was developed, in which fluorine-18 was introduced by substitution of a terminal tosyl group in the fatty acid backbone of GM1.
View Article and Find Full Text PDFMol Pharm
March 2020
Department of Nuclear Medicine, Molecular Imaging and Radiochemistry, Friedrich-Alexander University (FAU), Schwabachanlage 12, 91054 Erlangen, Germany.
The prostate-specific membrane antigen (PSMA) is a type II transmembrane glycoprotein that is highly expressed in the malignant human prostate epithelium. Therefore, PSMA has emerged as a very attractive target for developing radiopharmaceuticals for the diagnosis, e.g.
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