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@ARTICLE{Grner:1026693,
      author       = {Gröner, Benedikt and Hoffmann, Chris and Endepols, Heike
                      and Urusova, Elizaveta and Brugger, Melanie and Neumaier,
                      Felix and Timmer, Marco and Neumaier, Bernd and
                      Zlatopolskiy, Boris D.},
      title        = {{R}adiosynthesis and {P}reclinical {E}valuation of
                      m-[18{F}]{FET} and [18{F}]{FET}-{OM}e as {N}ovel
                      [18{F}]{FET} {A}nalogs for {B}rain {T}umor {I}maging},
      journal      = {Molecular pharmaceutics},
      volume       = {21},
      issn         = {1543-8384},
      address      = {Washington, DC},
      publisher    = {American Chemical Society},
      reportid     = {FZJ-2024-03507},
      pages        = {2795-2812},
      year         = {2024},
      note         = {This work was supported, in part, by
                      DeutscheForschungsgemeinschaft (DFG) grants ZL 65/1-1, ZL
                      65/3-1,and ZL 65/4-1.},
      abstract     = {O-([18F]Fluoroethyl)-L-tyrosine ([18F]FET) is
                      activelytransported into the brain and cancer cells by LAT1
                      andpossibly other amino acid transporters, which enables
                      brain tumorimaging by positron emission tomography (PET).
                      However, tumordelivery of this probe in the presence of
                      competing amino acidsmay be limited by a relatively low
                      affinity for LAT1. The aim of thepresent work was to
                      evaluate the meta-substituted [18F]FET analogm-[18F]FET and
                      the methyl ester [18F]FET-OMe, which weredesigned to improve
                      tumor delivery by altering the
                      physicochemical,pharmacokinetic, and/or transport
                      properties. Both tracerscould be prepared with good
                      radiochemical yields of $41−56\%within$ 66−90 min.
                      Preclinical evaluation with [18F]FET as areference tracer
                      demonstrated reduced in vitro uptake of [18F]FETOMeby U87
                      glioblastoma cells and no advantage for in vivo tumor
                      imaging. In contrast, m-[18F]FET showed significantly
                      improvedin vitro uptake and accelerated in vivo tumor
                      accumulation in an orthotopic glioblastoma model. As such,
                      our work identifies m-[18F]FET as a promising alternative to
                      [18F]FET for brain tumor imaging that deserves further
                      evaluation with regard to its transportproperties and in
                      vivo biodistribution.},
      cin          = {INM-5},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {5253 - Neuroimaging (POF4-525)},
      pid          = {G:(DE-HGF)POF4-5253},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {38747353},
      UT           = {WOS:001225916700001},
      doi          = {10.1021/acs.molpharmaceut.3c01215},
      url          = {https://juser.fz-juelich.de/record/1026693},
}