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@ARTICLE{Giesen:893828,
      author       = {Giesen, Beatriz and Nickel, Ann-Christin and Barthel, Juri
                      and Kahlert, Ulf Dietrich and Janiak, Christoph},
      title        = {{A}ugmented {T}herapeutic {P}otential of {G}lutaminase
                      {I}nhibitor {CB}839 in {G}lioblastoma {S}tem {C}ells {U}sing
                      {G}old {N}anoparticle {D}elivery},
      journal      = {Pharmaceutics},
      volume       = {13},
      number       = {2},
      issn         = {1999-4923},
      address      = {Basel},
      publisher    = {MDPI},
      reportid     = {FZJ-2021-02867},
      pages        = {295 -},
      year         = {2021},
      abstract     = {Gold nanoparticles (Au NPs) are studied as delivery systems
                      to enhance the effect of the glutaminase1 inhibitor CB839, a
                      promising drug candidate already in clinical trials for
                      tumor treatments. Au NPs were synthesized using a bottom-up
                      approach and covered with polymers able to bind CB839 as a
                      Au-polymer-CB839 conjugate. The drug loading efficiency
                      (DLE) was determined using high-performance liquid
                      chromatography and characterization of the CB839-loaded NPs
                      was done with various microscopic and spectroscopic methods.
                      Despite the chemical inertness of CB839, Au NPs were
                      efficient carriers with a DLE of up to $12\%,$ depending on
                      the polymer used. The therapeutic effect of CB839 with and
                      without Au was assessed in vitro in 2D and 3D glioblastoma
                      (GBM) cell models using different assays based on the colony
                      formation ability of GBM stem cells (GSCs). To avoid readout
                      disturbances from the Au metal, viability methods which do
                      not require optical detection were hereby optimized. These
                      showed that Au NP delivery increased the efficacy of CB839
                      in GSCs, compared to CB839 alone. Fluorescent microscopy
                      proved successful NP penetration into the GSCs. With this
                      first attempt to combine CB839 with Au nanotechnology, we
                      hope to overcome delivery hurdles of this pharmacotherapy
                      and increase bioavailability in target sites.},
      cin          = {ER-C-2},
      ddc          = {610},
      cid          = {I:(DE-Juel1)ER-C-2-20170209},
      pnm          = {5351 - Platform for Correlative, In Situ and Operando
                      Characterization (POF4-535) / 5353 - Understanding the
                      Structural and Functional Behavior of Solid State Systems
                      (POF4-535)},
      pid          = {G:(DE-HGF)POF4-5351 / G:(DE-HGF)POF4-5353},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {33672398},
      UT           = {WOS:000622975900001},
      doi          = {10.3390/pharmaceutics13020295},
      url          = {https://juser.fz-juelich.de/record/893828},
}