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@ARTICLE{Jiang:255501,
author = {Jiang, Nan and Leithold, Leonie H. E. and Post, Julia and
Ziehm, Tamar and Mauler, Jörg and Gremer, Lothar and
Cremer, Markus and Schartmann, Elena and Shah, N. J. and
Kutzsche, Janine and Langen, Karl-Josef and Breitkreutz,
Jörg and Willbold, Dieter and Willuweit, Antje},
title = {{P}reclinical {P}harmacokinetic {S}tudies of the {T}ritium
{L}abelled {D}-{E}nantiomeric {P}eptide {D}3 {D}eveloped for
the {T}reatment of {A}lzheimer´s {D}isease},
journal = {PLoS one},
volume = {10},
number = {6},
issn = {1932-6203},
address = {Lawrence, Kan.},
publisher = {PLoS},
reportid = {FZJ-2015-05663},
pages = {e0128553 -},
year = {2015},
abstract = {Targeting toxic amyloid beta (Aβ) oligomers is currently a
very attractive drug development strategy for treatment of
Alzheimer´s disease. Using mirror-image phage display
against Aβ1-42, we have previously identified the fully
D-enantiomeric peptide D3, which is able to eliminate Aβ
oligomers and has proven therapeutic potential in transgenic
Alzheimer´s disease animal models. However, there is little
information on the pharmacokinetic behaviour of
D-enantiomeric peptides in general. Therefore, we conducted
experiments with the tritium labelled D-peptide D3 (3H-D3)
in mice with different administration routes to study its
distribution in liver, kidney, brain, plasma and
gastrointestinal tract, as well as its bioavailability by
i.p. and p.o. administration. In addition, we investigated
the metabolic stability in liver microsomes, mouse plasma,
brain, liver and kidney homogenates, and estimated the
plasma protein binding. Based on its high stability and long
biological half-life, our pharmacokinetic results support
the therapeutic potential of D-peptides in general, with D3
being a new promising drug candidate for Alzheimer´s
disease treatment.},
cin = {INM-1 / INM-4 / ICS-6},
ddc = {500},
cid = {I:(DE-Juel1)INM-1-20090406 / I:(DE-Juel1)INM-4-20090406 /
I:(DE-Juel1)ICS-6-20110106},
pnm = {573 - Neuroimaging (POF3-573)},
pid = {G:(DE-HGF)POF3-573},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000355652200078},
pubmed = {pmid:26046986},
doi = {10.1371/journal.pone.0128553},
url = {https://juser.fz-juelich.de/record/255501},
}