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@ARTICLE{Kroth:23050,
author = {Kroth, H. and Ansaloni, A. and Varisco, Y. and Jan, A. and
Sreenivasachary, N. and Rezaei-Ghaleh, N. and Giriens, V.
and Lohmann, S. and Pilar López-Deber, M. and Adolfsson, O.
and Pihlgren, M. and Paganetti, P. and Froestl, W. and
Nagel-Steger, L. and Willbold, D and Schrader, T and
Zweckstetter, M. and Pfeifer, A. and Lashuel, H.A. and Muhs,
A.},
title = {{D}iscovery and structure activity relationship of small
molecule inhibitors of toxic-ß--amyloid-42 fibril
formation},
journal = {The journal of biological chemistry},
volume = {287},
issn = {0021-9258},
address = {Bethesda, Md.},
publisher = {Soc.},
reportid = {PreJuSER-23050},
pages = {34786 - 34800},
year = {2012},
note = {Record converted from VDB: 12.11.2012},
abstract = {Increasing evidence implicates Aβ peptides self-assembly
and fibril formation as crucial events in the pathogenesis
of Alzheimer disease. Thus, inhibiting Aβ aggregation,
among others, has emerged as a potential therapeutic
intervention for this disorder. Herein, we employed
3-aminopyrazole as a key fragment in our design of non-dye
compounds capable of interacting with Aβ42 via a
donor-acceptor-donor hydrogen bond pattern complementary to
that of the β-sheet conformation of Aβ42. The initial
design of the compounds was based on connecting two
3-aminopyrazole moieties via a linker to identify suitable
scaffold molecules. Additional aryl substitutions on the two
3-aminopyrazole moieties were also explored to enhance π-π
stacking/hydrophobic interactions with amino acids of Aβ42.
The efficacy of these compounds on inhibiting Aβ fibril
formation and toxicity in vitro was assessed using a
combination of biophysical techniques and viability assays.
Using structure activity relationship data from the in vitro
assays, we identified compounds capable of preventing
pathological self-assembly of Aβ42 leading to decreased
cell toxicity.},
cin = {ICS-6},
ddc = {570},
cid = {I:(DE-Juel1)ICS-6-20110106},
pnm = {Funktion und Dysfunktion des Nervensystems / BioSoft:
Makromolekulare Systeme und biologische
Informationsverarbeitung},
pid = {G:(DE-Juel1)FUEK409 / G:(DE-Juel1)FUEK505},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:22891248},
pmc = {pmc:PMC3464581},
UT = {WOS:000309654200078},
doi = {10.1074/jbc.M112.357665},
url = {https://juser.fz-juelich.de/record/23050},
}