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@ARTICLE{Morgenroth:834113,
      author       = {Morgenroth, Agnieszka and Vogg, Andreas T. J. and Neumaier,
                      Bernd and Mottaghy, Felix M. and Zlatopolskiy, Boris D.},
      title        = {{R}adioiodinated indomethacin amide for molecular imaging
                      of cyclooxygenase-2 expressing tumorsinm-5},
      journal      = {OncoTarget},
      volume       = {8},
      number       = {11},
      issn         = {1949-2553},
      address      = {[S.l.]},
      publisher    = {Impact Journals LLC},
      reportid     = {FZJ-2017-04114},
      pages        = {18059-18069},
      year         = {2017},
      abstract     = {Cyclooxygenase-2 (COX-2) is an important biomarker in
                      several tumors. Available imaging probes display relatively
                      low tumor to background ratios (smaller than 2:1). We
                      evaluated newly developed indomethacin (Ind) derivatives for
                      in vivo molecular imaging of COX-2 expressing carcinoma.
                      Radioiodinated Ind derivatives
                      Ind-NH-(CH2)4-NH-3-[I-125]I-Bz ([I-125]5),
                      Ind-NH-(CH2)4-NH-5-[I-124/125]I-Nic ([I-124/125]6) and
                      Ind-NH-(CH2)4-NH-5-[I-125]I-Iphth ([I-125]7) were prepared
                      from the respective SnBu3-precursors $(45–80\%$
                      radiochemical yield; > $95\%$ radiochemical purity). The
                      cellular uptake of [I-125]5 and [I-125]6 correlated with
                      COX-2 expression determined by SDS page/Western blot
                      analysis. [I-125]5 was predominantly localized in the cell
                      membrane while [I-125]6 was internalized and displayed a
                      diffuse and favorable cytoplasmic distribution. In contrast,
                      [I-125]7 showed only low uptake in COX-2 positive cells.
                      Co-incubation with the COX-2 inhibitor Celecoxib led to an
                      almost complete suppression of cellular uptake of [I-125]5
                      and [I-125]6. In vivo molecular imaging using positron
                      emission tomography (PET) in SCID mice xenografted with
                      COX-2+ (HT29) and COX-2− (HCT116) human colorectal
                      carcinoma cells was performed for [I-124]6. HT29 xenografts
                      displayed a significantly higher uptake than HCT-116
                      xenografts (5.6 ± 1.5 vs. 0.5 ± 0.1 kBq/g, P < 0.05) with
                      an extraordinary high tumor to muscle ratio (50.3 ± 1.5).
                      Immunohistological staining correlated with the imaging
                      data. In conclusion, the novel radioiodinated indomethacin
                      derivative ([I-124/125]6) could become a valuable tool for
                      development of molecular imaging probes for visualization of
                      COX-2 expressing tumors.},
      cin          = {INM-5},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {572 - (Dys-)function and Plasticity (POF3-572)},
      pid          = {G:(DE-HGF)POF3-572},
      typ          = {PUB:(DE-HGF)16},
      UT           = {WOS:000396877500053},
      doi          = {10.18632/oncotarget.15437},
      url          = {https://juser.fz-juelich.de/record/834113},
}