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@ARTICLE{Leveille:1044128,
      author       = {Leveille, Alexandria N. and Schwarzrock, Thomas and Brown,
                      Hawley and True, Bennett and Plasencia, Joanet and
                      Neudecker, Philipp and Üffing, Alina and Weiergräber,
                      Oliver H. and Willbold, Dieter and Kritzer, Joshua A.},
      title        = {{E}xploring {A}rylidene–{I}ndolinone {L}igands of
                      {A}utophagy {P}roteins {LC}3{B} and {GABARAP}},
      journal      = {ACS medicinal chemistry letters},
      volume       = {16},
      number       = {2},
      issn         = {1948-5875},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {FZJ-2025-03035},
      pages        = {271 - 277},
      year         = {2025},
      abstract     = {We report the first structure–activity studies of
                      arylidene–indolinone compound GW5074, which was reported
                      as a ligand of autophagy-related protein LC3B. The
                      literature has conflicting information on the binding
                      affinity of this compound, and there is some debate
                      regarding its use as a component of autophagy-dependent
                      degrader compounds. We developed an AlphaScreen assay to
                      measure competitive inhibition of the binding of known
                      peptide ligands to LC3B and its paralog GABARAP. Eighteen
                      analogs were synthesized and tested against both proteins.
                      Inhibitory potencies were found to be in the mid- to
                      high-micromolar range. 2D-NMR data revealed the binding site
                      on GABARAP as hydrophobic pocket 1, where native peptide
                      ligands bind with an aromatic side chain. Our results
                      suggest that GW5074 binds LC3B and GABARAP with micromolar
                      affinity. These affinities could support further exploration
                      in targeted protein degradation, but only if off-target
                      effects and poor solubility can be appropriately addressed.},
      cin          = {IBI-7},
      ddc          = {610},
      cid          = {I:(DE-Juel1)IBI-7-20200312},
      pnm          = {5241 - Molecular Information Processing in Cellular Systems
                      (POF4-524)},
      pid          = {G:(DE-HGF)POF4-5241},
      typ          = {PUB:(DE-HGF)16},
      doi          = {10.1021/acsmedchemlett.4c00517},
      url          = {https://juser.fz-juelich.de/record/1044128},
}