5-(2-18F-fluoroethoxy)-L-tryptophan as a substrate of system L transport for tumor imaging by PET

Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
Stefanie D KrämerSimon M Ametamey

Abstract

Large neutral l-amino acids are substrates of system L amino acid transporters. The level of one of these, LAT1, is increased in many tumors. Aromatic l-amino acids may also be substrates of aromatic l-amino acid decarboxylase (AADC), the level of which is enhanced in endocrine tumors. Increased amino acid uptake and subsequent decarboxylation result in the intracellular accumulation of the amino acid and its decarboxylation product. (18)F- and (11)C-labeled neutral aromatic amino acids, such as l-3,4-dihydroxy-6-(18)F-fluorophenylalanine ((18)F-FDOPA) and 5-hydroxy-l-[β-(11)C]tryptophan, are thus successfully used in PET to image endocrine tumors. However, 5-hydroxy-l-[β-(11)C]tryptophan has a relatively short physical half-life (20 min). In this work, we evaluated the in vitro and in vivo characteristics of the (18)F-labeled tryptophan analog 5-(2-(18)F-fluoroethoxy)-l-tryptophan ((18)F-l-FEHTP) as a PET probe for tumor imaging. (18)F-l-FEHTP was synthesized by no-carrier-added (18)F fluorination of 5-hydroxy-l-tryptophan. In vitro cell uptake and efflux of (18)F-l-FEHTP and (18)F-FDOPA were studied with NCI-H69 endocrine small cell lung cancer cells, PC-3 pseudoendocrine prostate cancer cells, and MDA-MB-231 exocrine breast ...Continue Reading

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Citations

Jul 16, 2013·International Journal of Pharmaceutics·Jeff Holst
Dec 7, 2013·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Adrienne MüllerStefanie D Krämer
Aug 20, 2014·BioMed Research International·I-Hong ShihDavid J Yang
Mar 20, 2013·Molecular Aspects of Medicine·Dimitrios FotiadisManuel Palacín
Nov 7, 2016·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Yangchun Xin, Hancheng Cai
Nov 21, 2015·Journal of Labelled Compounds & Radiopharmaceuticals·Małgorzata PająkMarianna Kańska
Sep 13, 2019·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Flóra JohnCsaba Juhász
Oct 25, 2016·Nuclear Medicine Communications·Shanzhen HeXiang Liang
Jun 3, 2015·Journal of Labelled Compounds & Radiopharmaceuticals·Cheol-Min YookJong Jin Lee
May 29, 2015·Clinical Nuclear Medicine·Sebastien DietemannAlessio Imperiale
Mar 1, 2019·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Yangchun XinHancheng Cai
Dec 9, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Peter RoseltLeonard I Wiebe
Oct 22, 2016·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Sharon K MichelhaughSandeep Mittal
Dec 18, 2013·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Alessio ImperialeDavid Taïeb
Jul 30, 2016·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Markus HuttererEugen Trinka

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