New fluoroethyl phenylalanine analogues as potential LAT1-targeting PET tracers for glioblastoma

Scientific Reports
Jeroen VerhoevenFilip De Vos

Abstract

The use of O-(2-[18F]fluoroethyl)-L-tyrosine ([18F]FET) as a positron emission tomography (PET) tracer for brain tumor imaging might have some limitations because of the relatively low affinity for the L-type amino acid transporter 1 (LAT1). To assess the stereospecificity and evaluate the influence of aromatic ring modification of phenylalanine LAT1 targeting tracers, six different fluoroalkylated phenylalanine analogues were synthesized. After in vitro Ki determination, the most promising compound, 2-[18F]-2-fluoroethyl-L-phenylalanine (2-[18F]FELP), was selected for further evaluation and in vitro comparison with [18F]FET. Subsequently, 2-[18F]FELP was assessed in vivo and compared with [18F]FET and [18F]FDG in a F98 glioblastoma rat model. 2-[18F]FELP showed improved in vitro characteristics over [18F]FET, especially when the affinity and specificity for system L is concerned. Based on our results, 2-[18F]FELP is a promising new PET tracer for brain tumor imaging.

References

Apr 27, 2002·European Journal of Nuclear Medicine and Molecular Imaging·Peter LavermanWim J G Oyen
Feb 18, 2003·European Journal of Nuclear Medicine and Molecular Imaging·Dirk PauleitKarl-J Langen
May 14, 2003·Neurochemistry International·Tobias HeckelStefan Bröer
Jul 2, 2003·Nuclear Medicine and Biology·Karl-Josef LangenHeinz H Coenen
May 27, 2005·Seminars in Cancer Biology·Bryan C Fuchs, Barrie P Bode
Mar 31, 2006·European Journal of Nuclear Medicine and Molecular Imaging·Veerle KersemansGuido Slegers
Aug 21, 2007·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Wei Chen
Jul 2, 2011·Nuclear Medicine and Biology·Thomas BourdierAndrew Katsifis
Jul 28, 2011·Medicinal Research Reviews·Jonathan McConathyMark M Goodman
Jan 21, 2012·Organic Letters·Jens WegnerIan R Baxendale
Jun 9, 2012·Neuro-oncology·Peter C HuszthyRolf Bjerkvig
Jun 30, 2012·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Pattama WiriyasermkulYoshikatsu Kanai
Mar 20, 2013·Molecular Aspects of Medicine·Dimitrios FotiadisManuel Palacín
Oct 26, 2013·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Norbert GalldiksKarl-Josef Langen
Jul 7, 2016·Angewandte Chemie·Jie WangPhil S Baran
Oct 19, 2016·International Journal of Molecular Sciences·Masahiro OnoHirokatsu Yoshimura
Dec 3, 2016·European Journal of Nuclear Medicine and Molecular Imaging·Chloé C FeralDavid Taïeb
Jan 25, 2017·NeuroImage. Clinical·Norbert GalldiksKarl-Josef Langen
Apr 8, 2017·Nature Reviews. Neurology·Karl-Josef LangenNadim Jon Shah
Feb 2, 2018·International Journal of Molecular Sciences·Stijn De MunterBart Vandekerckhove
Mar 12, 2018·Nuclear Medicine and Biology·Zhihao ZhaHank F Kung
Jul 27, 2018·Journal of Medicinal Chemistry·Huan-Chieh ChienAllen A Thomas

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Citations

Jun 9, 2020·Beilstein Journal of Organic Chemistry·Laila Fathy Awad, Mohammed Salah Ayoup
Jan 7, 2021·Cancers·Uğur KahyaAnna Dubrovska

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Methods Mentioned

BETA
flow cytometry
column chromatography
electrophoresis

Software Mentioned

miniGITA
GraphPad Prism
LabPET
GraphPad

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