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@ARTICLE{Oroz:140308,
author = {Oroz, Javier and Chang, Bliss J and Wysoczanski, Piotr and
Lee, Chung-Tien and Pérez-Lara, Ángel and Chakraborty,
Pijush and Hofele, Romina V and Baker, Jeremy D and Blair,
Laura J and Biernat, Jacek and Urlaub, Henning and
Mandelkow, Eckhard and Dickey, Chad A and Zweckstetter,
Markus},
title = {{S}tructure and pro-toxic mechanism of the human
{H}sp90/{PPI}ase/{T}au complex.},
journal = {Nature Communications},
volume = {9},
number = {1},
issn = {2041-1723},
address = {[London]},
publisher = {Nature Publishing Group UK},
reportid = {DZNE-2020-06630},
pages = {4532},
year = {2018},
abstract = {The molecular chaperone Hsp90 is critical for the
maintenance of cellular homeostasis and represents a
promising drug target. Despite increasing knowledge on the
structure of Hsp90, the molecular basis of substrate
recognition and pro-folding by Hsp90/co-chaperone complexes
remains unknown. Here, we report the solution structures of
human full-length Hsp90 in complex with the PPIase FKBP51,
as well as the 280 kDa Hsp90/FKBP51 complex bound to the
Alzheimer's disease-related protein Tau. We reveal that the
FKBP51/Hsp90 complex, which synergizes to promote toxic Tau
oligomers in vivo, is highly dynamic and stabilizes the
extended conformation of the Hsp90 dimer resulting in
decreased Hsp90 ATPase activity. Within the ternary
Hsp90/FKBP51/Tau complex, Hsp90 serves as a scaffold that
traps the PPIase and nucleates multiple conformations of
Tau's proline-rich region next to the PPIase catalytic
pocket in a phosphorylation-dependent manner. Our study
defines a conceptual model for dynamic
Hsp90/co-chaperone/client recognition.},
keywords = {Biocatalysis: drug effects / HSP90 Heat-Shock Proteins:
chemistry / HSP90 Heat-Shock Proteins: metabolism / HSP90
Heat-Shock Proteins: toxicity / Humans / Magnetic Resonance
Spectroscopy / Models, Molecular / Phosphorylation: drug
effects / Protein Binding: drug effects / Protein
Conformation / Tacrolimus Binding Proteins: chemistry /
Tacrolimus Binding Proteins: metabolism / Tacrolimus Binding
Proteins: toxicity / tau Proteins: chemistry / tau Proteins:
metabolism / tau Proteins: toxicity / HSP90 Heat-Shock
Proteins (NLM Chemicals) / tau Proteins (NLM Chemicals) /
Tacrolimus Binding Proteins (NLM Chemicals) / tacrolimus
binding protein 5 (NLM Chemicals)},
cin = {AG Zweckstetter / AG Mandelkow 1},
ddc = {500},
cid = {I:(DE-2719)1410001 / I:(DE-2719)1013014},
pnm = {342 - Disease Mechanisms and Model Systems (POF3-342)},
pid = {G:(DE-HGF)POF3-342},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:30382094},
pmc = {pmc:PMC6208366},
doi = {10.1038/s41467-018-06880-0},
url = {https://pub.dzne.de/record/140308},
}