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@ARTICLE{Brandt:301502,
      author       = {F. Brandt and M. Ullrich and M. Laube and R. Löser and J.
                      Kotzerke and K. Kopka$^*$ and J. Pietzsch and J. van den
                      Hoff and R. Wodtke},
      title        = {{D}eciphering the {T}umor {U}ptake of {H}eterobivalent
                      ({SST}2/{A}lbumin) [64{C}u]{C}u-{NODAGA}-c{LAB}-{TATE}s.},
      journal      = {Journal of medicinal chemistry},
      volume       = {68},
      number       = {11},
      issn         = {0095-9065},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {DKFZ-2025-01041},
      pages        = {12029-12046},
      year         = {2025},
      note         = {2025 Jun 12;68(11):12029-12046},
      abstract     = {Radioligands with albumin-binding moieties exhibit a great
                      potential for the treatment of tumor diseases owing to the
                      general finding of an increased integral tumor uptake
                      compared to radioligands without such moieties. However, the
                      reasons for this pharmacokinetic behavior are less explored.
                      Herein, we focused on identifying potential mechanisms for
                      our previously developed heterobivalent (SST2/albumin)
                      [64Cu]Cu-NODAGA-cLAB-TATEs. For this purpose, we designed
                      two novel derivatives that show either negligible binding to
                      albumin or lack the SST2-targeting capability. Based on the
                      in vivo results, we hypothesize that binding of the
                      albumin-bound radioligand to SST2 in addition to that of the
                      free radioligand causes the increased tumor uptake. This is
                      supported by saturation binding analyses in the presence of
                      albumin and compartment modeling considerations. Overall,
                      the results of this study provide a first tentative
                      explanation for the phenomenon of increased tumor uptake for
                      albumin-binding radioligands, which may support the
                      prospective design of such radioligands.},
      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:40393943},
      doi          = {10.1021/acs.jmedchem.5c00890},
      url          = {https://inrepo02.dkfz.de/record/301502},
}