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@ARTICLE{Yamanaka:136710,
author = {Yamanaka, Mitsugu and Ishikawa, Taizo and Griep, Angelika
and Axt, Daisy and Kummer, Markus P and Heneka, Michael T},
title = {{PPAR}γ/{RXR}α-induced and {CD}36-mediated microglial
amyloid-β phagocytosis results in cognitive improvement in
amyloid precursor protein/presenilin 1 mice.},
journal = {The journal of neuroscience},
volume = {32},
number = {48},
issn = {0270-6474},
address = {Washington, DC},
publisher = {Soc.57413},
reportid = {DZNE-2020-03032},
pages = {17321-17331},
year = {2012},
abstract = {Alzheimer's disease (AD) is characterized by the
extracellular deposition of amyloid-β (Aβ),
neurofibrillary tangle formation, and a microglial-driven
inflammatory response. Chronic inflammatory activation
compromises microglial clearance functions. Because
peroxisome proliferator-activated receptor γ (PPARγ)
agonists suppress inflammatory gene expression, we tested
whether activation of PPARγ would also result in improved
microglial Aβ phagocytosis. The PPARγ agonist pioglitazone
and a novel selective PPARα/γ modulator, DSP-8658,
currently in clinical development for the treatment of type
2 diabetes, enhanced the microglial uptake of Aβ in a
PPARγ-dependent manner. This PPARγ-stimulated increase of
Aβ phagocytosis was mediated by the upregulation of
scavenger receptor CD36 expression. In addition, combined
treatment with agonists for the heterodimeric binding
partners of PPARγ, the retinoid X receptors (RXRs), showed
additive enhancement of the Aβ uptake that was mediated by
RXRα activation. Evaluation of DSP-8658 in the amyloid
precursor protein/presenilin 1 mouse model confirmed an
increased microglial Aβ phagocytosis in vivo, which
subsequently resulted in a reduction of cortical and
hippocampal Aβ levels. Furthermore, DSP-8658-treated mice
showed improved spatial memory performance. Therefore,
stimulation of microglial clearance by simultaneous
activation of the PPARγ/RXRα heterodimer may prove
beneficial in prevention of AD.},
keywords = {Alzheimer Disease: drug therapy / Alzheimer Disease:
metabolism / Alzheimer Disease: psychology / Amyloid
beta-Protein Precursor: genetics / Amyloid beta-Protein
Precursor: metabolism / Animals / Behavior, Animal: drug
effects / Behavior, Animal: physiology / Brain: drug effects
/ Brain: metabolism / Cognition: drug effects / Cognition:
physiology / Disease Models, Animal / Hypoglycemic Agents:
pharmacology / Hypoglycemic Agents: therapeutic use / Maze
Learning: drug effects / Maze Learning: physiology / Mice /
Microglia: drug effects / Microglia: metabolism / PPAR
gamma: agonists / Phagocytosis: drug effects / Phagocytosis:
physiology / Pioglitazone / Presenilin-1: genetics /
Presenilin-1: metabolism / Thiazolidinediones: pharmacology
/ Thiazolidinediones: therapeutic use / Amyloid beta-Protein
Precursor (NLM Chemicals) / Hypoglycemic Agents (NLM
Chemicals) / PPAR gamma (NLM Chemicals) / Presenilin-1 (NLM
Chemicals) / Thiazolidinediones (NLM Chemicals) /
Pioglitazone (NLM Chemicals)},
cin = {Pre 2020 / AG Heneka2},
ddc = {610},
cid = {I:(DE-2719)999999 / I:(DE-2719)1011303},
pnm = {344 - Clinical and Health Care Research (POF3-344)},
pid = {G:(DE-HGF)POF3-344},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:23197723},
pmc = {pmc:PMC6621845},
doi = {10.1523/JNEUROSCI.1569-12.2012},
url = {https://pub.dzne.de/record/136710},
}