% IMPORTANT: The following is UTF-8 encoded. This means that in the presence % of non-ASCII characters, it will not work with BibTeX 0.99 or older. % Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or % “biber”. @ARTICLE{Schartmann:848233, author = {Schartmann, Elena and Schemmert, Sarah and Niemietz, Nicole and Honold, Dominik and Ziehm, Tamar and Tusche, Markus and Elfgen, Anne and Gering, Ian and Brener, Oleksandr and Shah, Nadim Joni and Langen, Karl-Josef and Kutzsche, Janine and Willbold, Dieter and Willuweit, Antje}, title = {{I}n {V}itro {P}otency and {P}reclinical {P}harmacokinetic {C}omparison of {A}ll-{D}-{E}nantiomeric {P}eptides {D}eveloped for the {T}reatment of {A}lzheimer’s {D}isease}, journal = {Journal of Alzheimer's disease}, volume = {64}, number = {3}, issn = {1387-2877}, address = {Amsterdam}, publisher = {IOS Press}, reportid = {FZJ-2018-03495}, pages = {859 - 873}, year = {2018}, abstract = {Diffusible amyloid-β (Aβ) oligomers are currently presumed to be the most cytotoxic Aβ assembly and held responsible to trigger the pathogenesis of Alzheimer’s disease (AD). Thus, Aβ oligomers are a prominent target in AD drug development. Previously, we reported on our solely D-enantiomeric peptide D3 and its derivatives as AD drug candidates. Here, we compare one of the most promising D3 derivatives, ANK6, with its tandem version (tANK6), and its head-to-tail cyclized isoform (cANK6r). In vitro tests investigating the D-peptides’ potencies to inhibit Aβ aggregation, eliminate Aβ oligomers, and reduce Aβ-induced cytotoxicity revealed that all three D-peptides efficiently target Aβ. Subsequent preclinical pharmacokinetic studies of the three all-D-peptides in wildtype mice showed promising blood-brain barrier permeability with cANK6r yielding the highest levels in brain. The peptides’ potencies to lower Aβ toxicity and their remarkable brain/plasma ratios make them promising AD drug candidates.}, cin = {ICS-6 / INM-4}, ddc = {610}, cid = {I:(DE-Juel1)ICS-6-20110106 / I:(DE-Juel1)INM-4-20090406}, pnm = {553 - Physical Basis of Diseases (POF3-553)}, pid = {G:(DE-HGF)POF3-553}, typ = {PUB:(DE-HGF)16}, pubmed = {pmid:29966196}, UT = {WOS:000437257500014}, doi = {10.3233/JAD-180165}, url = {https://juser.fz-juelich.de/record/848233}, }