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@ARTICLE{Schartmann:843818,
      author       = {Schartmann, Elena and Schemmert, Sarah and Ziehm, Tamar and
                      Leithold, Leonie H. E. and Jiang, Nan and Tusche, Markus and
                      Shah, N. J. and Langen, Karl-Josef and Kutzsche, Janine and
                      Willbold, Dieter and Willuweit, Antje},
      title        = {{C}omparison of blood-brain barrier penetration
                      efficiencies between linear and cyclic all- d -enantiomeric
                      peptides developed for the treatment of {A}lzheimer's
                      disease},
      journal      = {European journal of pharmaceutical sciences},
      volume       = {114},
      issn         = {0928-0987},
      address      = {New York, NY [u.a.]},
      publisher    = {Elsevier},
      reportid     = {FZJ-2018-01358},
      pages        = {93 - 102},
      year         = {2018},
      abstract     = {Alzheimer's disease (AD), until now, is an incurable
                      progressive neurodegenerative disease. To target toxic
                      amyloid β oligomers in AD patients' brains and to convert
                      them into non-toxic aggregation-incompetent species, we
                      designed peptides consisting solely of d-enantiomeric amino
                      acid residues. The original lead compound was named D3 and
                      several D3 derivatives were designed to enhance beneficial
                      properties. Here, we compare four d-peptides concerning
                      their efficiencies to pass the blood-brain barrier (BBB). We
                      demonstrate that the d-peptides' concentrations in murine
                      brain directly correlate with concentrations in
                      cerebrospinal fluid. The cyclic d-enantiomeric peptide
                      cRD2D3 is characterized by the highest efficiency to pass
                      the BBB. For in total three cyclic peptides we show that
                      administration of cyclic peptides resulted in up to tenfold
                      higher peak concentrations in brain as compared to their
                      linear equivalents which have partially been characterized
                      before (Jiang et al., 2015; Leithold et al., 2016a). These
                      results suggest that cyclic peptides pass the murine BBB
                      more efficiently than their linear equivalents. cRD2D3's
                      proteolytic stability, oral bioavailability, long duration
                      of action and its favorable brain/plasma ratio reveal that
                      it may become a suitable drug for long-term AD-treatment
                      from a pharmacokinetic point of view.},
      cin          = {INM-4 / ICS-6 / JARA-BRAIN},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-4-20090406 / I:(DE-Juel1)ICS-6-20110106 /
                      $I:(DE-82)080010_20140620$},
      pnm          = {573 - Neuroimaging (POF3-573)},
      pid          = {G:(DE-HGF)POF3-573},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:29225107},
      UT           = {WOS:000424977500011},
      doi          = {10.1016/j.ejps.2017.12.005},
      url          = {https://juser.fz-juelich.de/record/843818},
}