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@ARTICLE{Jin:300114,
      author       = {C. Jin and M. Emam and S. M. Klauck$^*$ and N. T. Ali and
                      R. Salem and W. M. Eldehna and T. Efferth and M. F. Hegazy
                      and M. Dawood},
      title        = {{T}argeting sensitive and multidrug resistant leukemia
                      cells with a novel benzofuran-isatin conjugate.},
      journal      = {European journal of pharmacology},
      volume       = {997},
      issn         = {0014-2999},
      address      = {New York, NY [u.a.]},
      publisher    = {Elsevier},
      reportid     = {DKFZ-2025-00612},
      pages        = {177538},
      year         = {2025},
      note         = {2025 Mar 22:997:177538},
      abstract     = {Benzofuran-isatin conjugates are considered as promising
                      compounds in cancer prevention and treatment. However, it is
                      not known yet whether these compounds are useful to
                      effectively treat multidrug-resistant tumors. In this study,
                      we investigated the activity of G-5e, a novel
                      benzofuran-isatin conjugate in a panel of cell lines
                      exhibiting well-known drug resistance mechanisms (P-gp,
                      BCRP, TP53, EGFR). P-glycoprotein overexpressing CEM/ADR5000
                      cell line displayed notable hypersensitivity (collateral
                      sensitivity) to G-5e, which was mediated through autophagic
                      cell death activation including downregulation of the
                      autophagy suppressor RND2, upregulation of the autophagy
                      inducer LC3B, and G0/G1 phase arrest during cell cycle
                      progression. Independent of collateral sensitivity,
                      transcriptomic analyses also revealed that G-5e caused
                      downregulation of NF-κB and ERK1/2 pathways. Our findings
                      highlight the potential of benzofuran-isatin conjugates to
                      combat multidrug resistance and the role of RND2 for
                      collateral sensitivity.},
      keywords     = {Autophagic cell death (Other) / Benzofuran-isatin conjugate
                      (Other) / Collateral sensitivity (Other) / Multidrug
                      resistance (Other) / P-glycoprotein (Other)},
      cin          = {B063},
      ddc          = {610},
      cid          = {I:(DE-He78)B063-20160331},
      pnm          = {312 - Funktionelle und strukturelle Genomforschung
                      (POF4-312)},
      pid          = {G:(DE-HGF)POF4-312},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:40122501},
      doi          = {10.1016/j.ejphar.2025.177538},
      url          = {https://inrepo02.dkfz.de/record/300114},
}