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@ARTICLE{Darwish:182156,
      author       = {S. Darwish and T. Heimburg and J. Ridinger$^*$ and D. Herp
                      and M. Schmidt and C. Romier and M. Jung and I. Oehme$^*$
                      and W. Sippl},
      title        = {{S}ynthesis, {B}iochemical, and {C}ellular {E}valuation of
                      {HDAC}6 {T}argeting {P}roteolysis {T}argeting {C}himeras.},
      journal      = {Methods in molecular biology},
      volume       = {2589},
      issn         = {1064-3745},
      address      = {[Heidelberg]},
      publisher    = {[Springer]},
      reportid     = {DKFZ-2022-02467},
      isbn         = {978-1-0716-2787-7 (print)},
      pages        = {179-193},
      year         = {2023},
      abstract     = {Histone deacetylases are considered promising epigenetic
                      targets for chemical protein degradation due to their
                      diverse roles in physiological cellular functions and in the
                      diseased state. Proteolysis-targeting chimeras (PROTACs) are
                      bifunctional molecules that hijack the cell's
                      ubiquitin-proteasome system (UPS). One of the promising
                      targets for this approach is histone deacetylase 6 (HDAC6),
                      which is highly expressed in several types of cancers and is
                      linked to the aggressiveness of tumors. In the present work,
                      we describe the synthesis of HDAC6 targeting PROTACs based
                      on previously synthesized benzohydroxamates selectively
                      inhibiting HDAC6 and how to assess their activities in
                      different biochemical in vitro assays and in cellular
                      assays. HDAC inhibition was determined using fluorometric
                      assays, while the degradation ability of the PROTACs was
                      assessed using western blot analysis.},
      keywords     = {Epigenetic proteins (Other) / Histone deacetylase 6 (Other)
                      / Proteolysis-targeting chimeras (Other)},
      cin          = {B310 / HD01},
      ddc          = {570},
      cid          = {I:(DE-He78)B310-20160331 / I:(DE-He78)HD01-20160331},
      pnm          = {312 - Funktionelle und strukturelle Genomforschung
                      (POF4-312)},
      pid          = {G:(DE-HGF)POF4-312},
      typ          = {PUB:(DE-HGF)3 / PUB:(DE-HGF)16},
      pubmed       = {pmid:36255625},
      doi          = {10.1007/978-1-0716-2788-4_12},
      url          = {https://inrepo02.dkfz.de/record/182156},
}