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@ARTICLE{Seyfert:603154,
      author       = {Seyfert, Carsten E. and Müller, Alison V. and Walsh,
                      Danica J. and Birkelbach, Joy and Kany, Andreas M. and
                      Porten, Christoph and Yuan, Biao and Krug, Daniel and
                      Herrmann, Jennifer and Marlovits, Thomas and Hirsch, Anna K.
                      H. and Müller, Rolf},
      title        = {{N}ew {G}enetically {E}ngineered {D}erivatives of
                      {A}ntibacterial {D}arobactins {U}nderpin {T}heir {P}otential
                      for {A}ntibiotic {D}evelopment},
      journal      = {Journal of medicinal chemistry},
      volume       = {66},
      number       = {23},
      issn         = {0095-9065},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {PUBDB-2024-00791},
      pages        = {16330 - 16341},
      year         = {2023},
      note         = {Helmholtz Validation Funds and Gottfried-Wilhem Leibniz
                      Preis der Deutschen Forschungsgemeinschaft (DFG) MU
                      1254/32-1 are acknowledged.},
      abstract     = {Biosynthetic engineering of bicyclic darobactins,
                      selectively sealing the lateral gate of the outer membrane
                      protein BamA, leads to active analogues, which are up to
                      128-fold more potent against Gram-negative pathogens
                      compared to native counterparts. Because of their excellent
                      antibacterial activity, darobactins represent one of the
                      most promising new antibiotic classes of the past decades.
                      Here, we present a series of structure-driven biosynthetic
                      modifications of our current frontrunner, darobactin 22
                      (D22), to investigate modifications at the understudied
                      positions 2, 4, and 5 for their impact on bioactivity. Novel
                      darobactins were found to be highly active against critical
                      pathogens from the WHO priority list. Antibacterial activity
                      data were corroborated by dissociation constants with BamA.
                      The most active derivatives D22 and D69 were subjected to
                      ADMET profiling, showing promising features. We further
                      evaluated D22 and D69 for bioactivity against
                      multidrug-resistant clinical isolates and found them to have
                      strong activity.},
      cin          = {CSSB-UKE-TM},
      ddc          = {610},
      cid          = {I:(DE-H253)CSSB-UKE-TM-20210520},
      pnm          = {633 - Life Sciences – Building Blocks of Life: Structure
                      and Function (POF4-633)},
      pid          = {G:(DE-HGF)POF4-633},
      experiment   = {EXP:(DE-MLZ)NOSPEC-20140101},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:38093695},
      UT           = {WOS:001142969500001},
      doi          = {10.1021/acs.jmedchem.3c01660},
      url          = {https://bib-pubdb1.desy.de/record/603154},
}