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@ARTICLE{Lis:300143,
      author       = {C. Lis and F.-A. Ludwig and S. Fischer and M. Ullrich and
                      H.-J. Lankau and W. Sihver and D. Gündel and D. Joseph and
                      C. Meyer and K. Kopka$^*$ and J. Pietzsch and P. Brust and
                      A. Hoepping},
      title        = {{D}evelopment of [99m{T}c]{T}c{O}-{ABX}474: {D}esign,
                      {S}ynthesis, and {B}iological {E}valuation of
                      {PSMA}-{B}inding {T}echnetium-99m {R}adioligands for {SPECT}
                      {I}maging of {P}rostate {C}ancer.},
      journal      = {Journal of medicinal chemistry},
      volume       = {68},
      number       = {7},
      issn         = {0095-9065},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {DKFZ-2025-00634},
      pages        = {7213-7231},
      year         = {2025},
      note         = {2025 Apr 10;68(7):7213-7231},
      abstract     = {A current global limitation to the timely and equitable
                      patient access to PSMA-based therapies for prostate cancer
                      (PCa) is the insufficient PET capacity for pretreatment
                      imaging. However, the extensive global availability of SPECT
                      cameras renders this imaging technology as an attractive
                      alternative. The lack of regulatory approved PSMA
                      radioligands for SPECT imaging of PCa prompted us to design
                      new 99mTc-labeled radioligands with a fast pharmacokinetic
                      profile by harnessing proven complexation of the
                      [99mTc][TcO]3+ core by a bis(aminoethanethiol) chelator. Six
                      99mTc-labeled PSMA radioligands were synthesized and
                      biologically characterized in cell-based assays and by SPECT
                      imaging in LNCaP tumor-bearing mice. From this series,
                      [99mTc]TcO-5 ([99mTc]TcO-ABX474, Kd(PSMA) = 6.1 ± 1.7 nM)
                      displayed the most advantageous properties for SPECT imaging
                      of PCa: high and fast tumor uptake accompanied by rapid
                      clearance from nontarget tissues, leading to faster
                      pharmacokinetics than observed for the reference
                      $[99mTc]Tc-PSMA-I\&S.$ Furthermore, [99mTc]TcO-5 performed
                      similar to the established PSMA-PET radioligand
                      [68Ga]Ga-PSMA-11.},
      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:40135799},
      doi          = {10.1021/acs.jmedchem.4c02767},
      url          = {https://inrepo02.dkfz.de/record/300143},
}