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@ARTICLE{Feni:842598,
      author       = {Feni, Lucia and Omrane, Aymen and Fischer, Moritz and
                      Zlatopolskiy, Boris and Neumaier, Bernd and Neundorf, Ines},
      title        = {{C}onvenient {P}reparation of 18{F}-{L}abeled {P}eptide
                      {P}robes for {P}otential {C}laudin-4 {PET} {I}maging},
      journal      = {Pharmaceuticals},
      volume       = {10},
      number       = {4},
      issn         = {1424-8247},
      address      = {Basel},
      publisher    = {MDPI},
      reportid     = {FZJ-2018-00811},
      pages        = {99 -},
      year         = {2017},
      abstract     = {Since pancreatic cancer is often diagnosed in a late state
                      of cancer development, diagnostic opportunities allowing
                      early disease detection are highly sought after. As such,
                      cancer expression of claudin proteins is markedly
                      dysregulated, making it an attractive target for molecular
                      imaging like positron emission tomography (PET). Claudins
                      are a family of transmembrane proteins that have a pivotal
                      role as members of the tight junctions. In particular,
                      claudin-3 and claudin-4 are frequently overexpressed in
                      pancreatic cancer. 18F-Labeled claudin selective peptides
                      would provide access to a novel kind of imaging tools for
                      pancreatic cancer. In this work we describe the synthesis of
                      the first 18F-labeled probes potentially suitable for PET
                      imaging of claudin-4 expression. These probes were prepared
                      using oxime ligation of 5-[18F]fluoro-5-deoxyribose
                      (5-[18F]FDR) to claudin selective peptides. As a
                      proof-of-principle, one of them, 5-[18F]FDR-Clone 27, was
                      isolated in $>98\%$ radiochemical purity and in $15\%$
                      radiochemical yield (EOB) within 98 min, and with a molar
                      activity of 4.0 GBq/μmol (for 30 MBq of tracer). Moreover,
                      we present first biological data for the prepared
                      5-FDR-conjugates. These tracers could pave the way for an
                      early diagnosis of pancreatic tumor, and thus improve the
                      outcome of anticancer therapy.},
      cin          = {INM-5},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {573 - Neuroimaging (POF3-573)},
      pid          = {G:(DE-HGF)POF3-573},
      typ          = {PUB:(DE-HGF)16},
      UT           = {WOS:000419241100021},
      pubmed       = {pmid:29258264},
      doi          = {10.3390/ph10040099},
      url          = {https://juser.fz-juelich.de/record/842598},
}