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@ARTICLE{Kutzsche:838455,
      author       = {Kutzsche, Janine and Schemmert, Sarah and Tusche, Markus
                      and Neddens, J. and Rabl, R. and Jürgens, Dagmar and
                      Brener, O. and Willuweit, Antje and Hutter-Paier, B. and
                      Willbold, Dieter},
      title        = {{L}arge-{S}cale {O}ral {T}reatment {S}tudy with the {F}our
                      {M}ost {P}romising {D}3-{D}erivatives for the {T}reatment of
                      {A}lzheimer’s {D}isease},
      journal      = {Molecules},
      volume       = {22},
      issn         = {1420-3049},
      address      = {Basel},
      publisher    = {MDPI},
      reportid     = {FZJ-2017-07058},
      pages        = {1693},
      year         = {2017},
      abstract     = {Alzheimer’s disease (AD) is a progressive
                      neurodegenerative disorder that is associated with the
                      aggregation of the amyloid β protein (Aβ). Aβ oligomers
                      are currently thought to be the major neurotoxic agent
                      responsible for disease development and progression. Thus,
                      their elimination is highly desirable for therapy
                      development. Our therapeutic approach aims at specific and
                      direct elimination of toxic Aβ oligomers by stabilizing Aβ
                      monomers in an aggregation-incompetent conformation. We have
                      proven that our lead compound “D3”, an all
                      d-enantiomeric-peptide, specifically eliminates Aβ
                      oligomers in vitro. In vivo, D3 enhances cognition and
                      reduces plaque load in several transgenic AD mouse models.
                      Here, we performed a large-scale oral proof of concept
                      efficacy study, in which we directly compared four of the
                      most promising D3-derivatives in transgenic mice expressing
                      human amyloid precursor protein with Swedish and London
                      mutations (APPSL), transgenic mice, to identify the most
                      effective compound. RD2 and D3D3, both derived from D3 by
                      rational design, were discovered to be the most effective
                      derivatives in improving cognition in the Morris water maze.
                      The performance of RD2- and D3D3-treated mice within the
                      Morris water maze was significantly better than
                      placebo-treated mice and, importantly, nearly as good as
                      those of non-transgenic littermates, suggesting a complete
                      reversal of the cognitive deficit of APPSL mice.},
      cin          = {ICS-6},
      ddc          = {540},
      cid          = {I:(DE-Juel1)ICS-6-20110106},
      pnm          = {553 - Physical Basis of Diseases (POF3-553)},
      pid          = {G:(DE-HGF)POF3-553},
      typ          = {PUB:(DE-HGF)16},
      UT           = {WOS:000414670600120},
      pubmed       = {pmid:28994710},
      doi          = {10.3390/molecules22101693},
      url          = {https://juser.fz-juelich.de/record/838455},
}