radionuclide-fluorescence-reporter-gene-imaging-to-track-tumor

Radionuclide-fluorescence Reporter Gene Imaging to Track Tumor Progression in Rodent Tumor Models

Metastasis is responsible for most cancer deaths. Despite extensive research, the mechanistic understanding of the complex processes governing metastasis ...

King's College London

[(18)F]BF4 (-), the first (18)F-labelled PET imaging agent for the sodium/iodide symporter (NIS), was produced by isotopic exchange yielding a product with limited specific activity (SA, ca. 1 GBq/μmol) posing a risk of sub-optimal target-to-background ratios (TBR) in PET images due to saturation of NIS in vivo. We sought to quantify this risk and to develop a method of production of [(18)F]BF4 (-) with higher SA.

[(18)F]tetrafluoroborate as a PET tracer for the sodium/iodide symporter: the importance of specific activity.

Anion transport by the human sodium-iodide symporter (hNIS) is an established target for molecular imaging and radionuclide therapy. Current radiotracers for PET of hNIS expression are limited toIandF-BFWe sought newF-labeled hNIS substrates offering higher specific activity, higher affinity, and simpler radiochemical synthesis thanF-BFMETHODS: The ability of a range of anions, some containing fluorine, to blockTcOuptake in hNIS-expressing cells was measured. SOFemerged as a promising candidate.F-SOFwas synthesized by reaction ofFwith SO-pyridine complex in MeCN and purified using alumina and quaternary methyl ammonium solid-phase extraction cartridges. Chemical and radiochemical purity and serum stability were determined by radiochromatography. Radiotracer uptake and efflux in hNIS-transduced HCT116-C19 cells and the hNIS-negative parent cell line were evaluated in vitro in the presence and absence of a known competitive inhibitor (NaClO). PET/CT imaging and ex vivo biodistribution measurement were conducted on BALB/c mice, with and without NaClOinhibition.

Article	Year
[(18)F]tetrafluoroborate as a PET tracer for the sodium/iodide symporter: the importance of specific activity. EJNMMI research\| PubMed ID: 27103614	2016
18F-Fluorosulfate for PET Imaging of the Sodium-Iodide Symporter: Synthesis and Biologic Evaluation In Vitro and In Vivo. Journal of nuclear medicine : official publication, Society of Nuclear Medicine\| PubMed ID: 27539841	2017

Alex Khoshnevisan

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