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@ARTICLE{Brandt:186568,
      author       = {F. Brandt and M. Ullrich and J. Wodtke and K. Kopka$^*$ and
                      M. Bachmann and R. Löser and J. Pietzsch and H.-J. Pietzsch
                      and R. Wodtke},
      title        = {{E}nzymological {C}haracterization of 64{C}u-{L}abeled
                      {N}eprilysin {S}ubstrates and {T}heir {A}pplication for
                      {M}odulating the {R}enal {C}learance of {T}argeted
                      {R}adiopharmaceuticals.},
      journal      = {Journal of medicinal chemistry},
      volume       = {66},
      number       = {1},
      issn         = {0095-9065},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {DKFZ-2023-00017},
      pages        = {516-537},
      year         = {2023},
      note         = {2023 Jan 12;66(1):516-537},
      abstract     = {The applicability of radioligands for targeted
                      endoradionuclide therapy is limited due to radiation-induced
                      toxicity to healthy tissues, in particular to the kidneys as
                      primary organs of elimination. The targeting of enzymes of
                      the renal brush border membrane by cleavable linkers that
                      permit the formation of fast eliminating
                      radionuclide-carrying cleavage fragments gains increasing
                      interest. Herein, we synthesized a small library of
                      64Cu-labeled cleavable linkers and quantified their
                      substrate potentials toward neprilysin (NEP), a highly
                      abundant peptidase at the renal brush border membrane. This
                      allowed for the derivation of structure-activity
                      relationships, and selected cleavable linkers were attached
                      to the somatostatin receptor subtype 2 ligand
                      [Tyr3]octreotate. Radiopharmacological characterization
                      revealed that a substrate-based targeting of NEP in the
                      kidneys with small peptides entails their premature cleavage
                      in the blood circulation by soluble and endothelium-derived
                      NEP. However, for a kidney-specific targeting of NEP, the
                      additional targeting of albumin in the blood is
                      highlighted.},
      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:36595224},
      doi          = {10.1021/acs.jmedchem.2c01472},
      url          = {https://inrepo02.dkfz.de/record/186568},
}