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@ARTICLE{Krutzek:276071,
      author       = {F. Krutzek and C. K. Donat and M. Ullrich and K. Zarschler
                      and M.-C. Ludik and A. Feldmann and L. R. Loureiro and K.
                      Kopka$^*$ and S. Stadlbauer},
      title        = {{D}esign and {B}iological {E}valuation of
                      {S}mall-{M}olecule {PET}-{T}racers for {I}maging of
                      {P}rogrammed {D}eath {L}igand 1.},
      journal      = {Cancers},
      volume       = {15},
      number       = {9},
      issn         = {2072-6694},
      address      = {Basel},
      publisher    = {MDPI},
      reportid     = {DKFZ-2023-00977},
      pages        = {2638},
      year         = {2023},
      abstract     = {Noninvasive molecular imaging of the PD-1/PD-L1 immune
                      checkpoint is of high clinical relevance for patient
                      stratification and therapy monitoring in cancer patients.
                      Here we report nine small-molecule PD-L1 radiotracers with
                      solubilizing sulfonic acids and a linker-chelator system,
                      designed by molecular docking experiments and synthesized
                      according to a new, convergent synthetic strategy. Binding
                      affinities were determined both in cellular saturation and
                      real-time binding assay (LigandTracer), revealing
                      dissociation constants in the single digit nanomolar range.
                      Incubation in human serum and liver microsomes proved in
                      vitro stability of these compounds. Small animal PET/CT
                      imaging, in mice bearing PD-L1 overexpressing and PD-L1
                      negative tumors, showed moderate to low uptake. All
                      compounds were cleared primarily through the hepatobiliary
                      excretion route and showed a long circulation time. The
                      latter was attributed to strong blood albumin binding
                      effects, discovered during our binding experiments. Taken
                      together, these compounds are a promising starting point for
                      further development of a new class of PD-L1 targeting
                      radiotracers.},
      keywords     = {PD-L1 (Other) / PET imaging (Other) / immune checkpoint
                      inhibitors (Other) / organic synthesis (Other) / radiotracer
                      (Other) / small molecules (Other)},
      cin          = {DD01},
      ddc          = {610},
      cid          = {I:(DE-He78)DD01-20160331},
      pnm          = {899 - ohne Topic (POF4-899)},
      pid          = {G:(DE-HGF)POF4-899},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:37174103},
      pmc          = {pmc:PMC10177516},
      doi          = {10.3390/cancers15092638},
      url          = {https://inrepo02.dkfz.de/record/276071},
}