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@ARTICLE{Tas:289902,
      author       = {H. Tas$^*$ and G. Bakos$^*$ and U. Bauder-Wüst$^*$ and M.
                      Schäfer$^*$ and Y. Remde$^*$ and M. Roscher$^*$ and M.
                      Benesova-Schäfer$^*$},
      title        = {{H}uman {ABC} and {SLC} {T}ransporters: {T}he {C}ulprit
                      {R}esponsible for {U}nspecific {PSMA}-617 {U}ptake?},
      journal      = {Pharmaceuticals},
      volume       = {17},
      number       = {4},
      issn         = {1424-8247},
      address      = {Basel},
      publisher    = {MDPI},
      reportid     = {DKFZ-2024-00894},
      pages        = {513},
      year         = {2024},
      note         = {#EA:E270#LA:E270#},
      abstract     = {[177Lu]Lu-PSMA-617 has recently been successfully approved
                      by the FDA, the MHRA, Health Canada and the EMA as
                      Pluvicto®. However, salivary gland (SG) and kidney
                      toxicities account for its main dose-limiting side-effects,
                      while its corresponding uptake and retention mechanisms
                      still remain elusive. Recently, the presence of different
                      ATP-binding cassette (ABC) transporters, such as human
                      breast cancer resistance proteins (BCRP), multidrug
                      resistance proteins (MDR1), multidrug-resistance-related
                      proteins (MRP1, MRP4) and solute cassette (SLC)
                      transporters, such as multidrug and toxin extrusion proteins
                      (MATE1, MATE2-K), organic anion transporters (OAT1, OAT2v1,
                      OAT3, OAT4) and peptide transporters (PEPT2), has been
                      verified at different abundances in human SGs and kidneys.
                      Therefore, our aim was to assess whether [177Lu]Lu-PSMA-617
                      and [225Ac]Ac-PSMA-617 are substrates of these ABC and SLC
                      transporters. For in vitro studies, the novel isotopologue
                      ([α,β-3H]Nal)Lu-PSMA-617 was used in cell lines or
                      vesicles expressing the aforementioned human ABC and SLC
                      transporters for inhibition and uptake studies,
                      respectively. The corresponding probe substrates and
                      reference inhibitors were used as controls. Our results
                      indicate that [177Lu]Lu-PSMA-617 and [225Ac]Ac-PSMA-617 are
                      neither inhibitors nor substrates of the examined
                      transporters. Therefore, our results show that human ABC and
                      SLC transporters play no central role in the uptake and
                      retention of [177Lu]Lu-PSMA-617 and [225Ac]Ac-PSMA-617 in
                      the SGs and kidneys nor in the observed toxicities.},
      keywords     = {PSMA (Other) / PSMA-617 (Other) / efflux transporters
                      (Other) / kidney toxicity (Other) / prostate cancer (Other)
                      / salivary gland toxicity (Other) / side-effects (Other) /
                      targeted alpha therapy (Other) / targeted radionuclide
                      therapy (Other) / uptake transporters (Other)},
      cin          = {E270 / W630},
      ddc          = {610},
      cid          = {I:(DE-He78)E270-20160331 / I:(DE-He78)W630-20160331},
      pnm          = {315 - Bildgebung und Radioonkologie (POF4-315)},
      pid          = {G:(DE-HGF)POF4-315},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:38675472},
      pmc          = {pmc:PMC11053447},
      doi          = {10.3390/ph17040513},
      url          = {https://inrepo02.dkfz.de/record/289902},
}