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@ARTICLE{Wagner:138181,
author = {Wagner, Jens and Krauß, Sybille and Shi, Song and
Ryazanov, Sergey and Steffen, Julia and Miklitz, Carolin and
Leonov, Andrei and Kleinknecht, Alexander and Göricke,
Bettina and Weishaupt, Jochen H and Weckbecker, Daniel and
Reiner, Anne M and Zinth, Wolfgang and Levin, Johannes and
Ehninger, Dan and Remy, Stefan and Kretzschmar, Hans A and
Griesinger, Christian and Giese, Armin and Fuhrmann, Martin},
title = {{R}educing tau aggregates with anle138b delays disease
progression in a mouse model of tauopathies.},
journal = {Acta neuropathologica},
volume = {130},
number = {5},
issn = {0001-6322},
address = {Heidelberg},
publisher = {Springer},
reportid = {DZNE-2020-04503},
pages = {619-631},
year = {2015},
abstract = {Pathological tau aggregation leads to filamentous tau
inclusions and characterizes neurodegenerative tauopathies
such as Alzheimer's disease and frontotemporal dementia and
parkinsonism linked to chromosome 17. Tau aggregation
coincides with clinical symptoms and is thought to mediate
neurodegeneration. Transgenic mice overexpressing mutant
human P301S tau exhibit many neuropathological features of
human tauopathies including behavioral deficits and
increased mortality. Here, we show that the
di-phenyl-pyrazole anle138b binds to aggregated tau and
inhibits tau aggregation in vitro and in vivo. Furthermore,
anle138b treatment effectively ameliorates disease symptoms,
increases survival time and improves cognition of tau
transgenic PS19 mice. In addition, we found decreased
synapse and neuron loss accompanied by a decreased gliosis
in the hippocampus. Our results suggest that reducing tau
aggregates with anle138b may represent an effective and
promising approach for the treatment of human tauopathies.},
keywords = {Animals / Benzodioxoles: pharmacology / Cell Death: drug
effects / Cell Death: physiology / Disease Models, Animal /
Disease Progression / Female / Gliosis: drug therapy /
Gliosis: pathology / Gliosis: physiopathology / Hippocampus:
drug effects / Hippocampus: pathology / Hippocampus:
physiopathology / Male / Mice, Transgenic / Motor Activity:
drug effects / Motor Activity: physiology / Neurons: drug
effects / Neurons: pathology / Neurons: physiology /
Neuroprotective Agents: pharmacology / Protein Aggregates:
drug effects / Pyrazoles: pharmacology / Random Allocation /
Recognition, Psychology: drug effects / Recognition,
Psychology: physiology / Tauopathies: drug therapy /
Tauopathies: pathology / tau Proteins: genetics / tau
Proteins: metabolism /
3-(1,3-benzodioxol-5-yl)-5-(3-bromophenyl)-1H-pyrazole (NLM
Chemicals) / Benzodioxoles (NLM Chemicals) / MAPT protein,
human (NLM Chemicals) / Mapt protein, mouse (NLM Chemicals)
/ Neuroprotective Agents (NLM Chemicals) / Protein
Aggregates (NLM Chemicals) / Pyrazoles (NLM Chemicals) / tau
Proteins (NLM Chemicals)},
cin = {AG Fuhrmann / AG Krauß / AG Remy / AG Ehninger},
ddc = {610},
cid = {I:(DE-2719)1011004 / I:(DE-2719)1011006 /
I:(DE-2719)1013006 / I:(DE-2719)1013005},
pnm = {341 - Molecular Signaling (POF3-341) / 342 - Disease
Mechanisms and Model Systems (POF3-342)},
pid = {G:(DE-HGF)POF3-341 / G:(DE-HGF)POF3-342},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:26439832},
pmc = {pmc:PMC4612332},
doi = {10.1007/s00401-015-1483-3},
url = {https://pub.dzne.de/record/138181},
}