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 Repjournal_title
Scientific reportsauthors
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 Fdoi
10.1038/s41598-019-40013-xsubject
Has Abstractpub_date
2019-02-27 00:00:00pages
2878issue
1issn
2045-2322pii
10.1038/s41598-019-40013-xjournal_volume
9pub_type
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