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

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.

journal_name

Sci Rep

journal_title

Scientific reports

authors

Verhoeven J,Hulpia F,Kersemans K,Bolcaen J,De Lombaerde S,Goeman J,Descamps B,Hallaert G,Van den Broecke C,Deblaere K,Vanhove C,Van der Eycken J,Van Calenbergh S,Goethals I,De Vos F

doi

10.1038/s41598-019-40013-x

subject

Has Abstract

pub_date

2019-02-27 00:00:00

pages

2878

issue

1

issn

2045-2322

pii

10.1038/s41598-019-40013-x

journal_volume

9

pub_type

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