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@ARTICLE{Ng:274581,
      author       = {Y. L. D. Ng and A. Bricelj and J. A. Jansen and A.
                      Murgai$^*$ and K. Peter and K. A. Donovan and M. Gütschow
                      and J. Krönke$^*$ and C. Steinebach and I. Sosič},
      title        = {{H}eterobifunctional {L}igase {R}ecruiters {E}nable
                      pan-{D}egradation of {I}nhibitor of {A}poptosis {P}roteins.},
      journal      = {Journal of medicinal chemistry},
      volume       = {66},
      number       = {7},
      issn         = {0095-9065},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {DKFZ-2023-00658},
      pages        = {4703-4733},
      year         = {2023},
      note         = {2023 Apr 13;66(7):4703-4733},
      abstract     = {Proteolysis targeting chimeras (PROTACs) represent a new
                      pharmacological modality to inactivate disease-causing
                      proteins. PROTACs operate via recruiting E3 ubiquitin
                      ligases, which enable the transfer of ubiquitin tags onto
                      their target proteins, leading to proteasomal degradation.
                      However, several E3 ligases are validated pharmacological
                      targets themselves, of which inhibitor of apoptosis (IAP)
                      proteins are considered druggable in cancer. Here, we report
                      three series of heterobifunctional PROTACs, which consist of
                      an IAP antagonist linked to either von Hippel-Lindau- or
                      cereblon-recruiting ligands. Hijacking E3 ligases against
                      each other led to potent, rapid, and preferential depletion
                      of cellular IAPs. In addition, these compounds caused
                      complete X-chromosome-linked IAP knockdown, which was rarely
                      observed for monovalent and homobivalent IAP antagonists. In
                      cellular assays, hit degrader 9 outperformed antagonists and
                      showed potent inhibition of cancer cell viability. The
                      hetero-PROTACs disclosed herein are valuable tools to
                      facilitate studies of the biological roles of IAPs and will
                      stimulate further efforts toward E3-targeting therapies.},
      cin          = {BE01},
      ddc          = {610},
      cid          = {I:(DE-He78)BE01-20160331},
      pnm          = {899 - ohne Topic (POF4-899)},
      pid          = {G:(DE-HGF)POF4-899},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:36996313},
      doi          = {10.1021/acs.jmedchem.2c01817},
      url          = {https://inrepo02.dkfz.de/record/274581},
}