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@ARTICLE{DiLorenzo:281530,
author = {Di Lorenzo, Davide and Bisi, Nicolo and Kaffy, Julia and
Ramirez, Lisa Marie and Zweckstetter, Markus and Lequin,
Olivier and Garfagnini, Irene and Luo, Jinghui and
Hannappel, Yvonne and Ennen, Inga and Dodero, Veronica and
Sewald, Norbert and Gelmi, Maria Luisa and Tonali, Nicolo
and Brandt, Roland and Ongeri, Sandrine},
title = {{S}ynthetic chaperone based on {H}sp90-{T}au interaction
inhibits {T}au aggregation and rescues physiological
{T}au-{M}icrotubule interaction.},
journal = {Nature Communications},
volume = {16},
number = {1},
issn = {2041-1723},
address = {[London]},
publisher = {Springer Nature},
reportid = {DZNE-2025-01148},
pages = {8756},
year = {2025},
abstract = {The accumulation of intracellular aggregates of Tau protein
is one main hallmark of Alzheimer's disease (AD) and is the
consequence of Tau conformational changes, increased
phosphorylation, and self-association to form fibrillar
aggregates. This pathological process prevents the
physiological interaction of Tau with microtubules to the
detriment of the structural integrity of neurons. In healthy
cells, aberrant protein misfolding and aggregation are
counteracted by chaperone proteins whose protective capacity
decreases with age. The role of the chaperone Hsp90 and the
mechanism by which it can prevent Tau aggregation are
controversial. In this work, the strategy of mimicking Hsp90
through the design of the β-hairpin like peptidomimetic
β-Hsp90, inspired by two Hsp90/Tau interaction sequences,
is presented. β-Hsp90 inhibits Tau aggregation both in
vitro and in cells, restoring Tau's physiological
interaction with microtubules. β-Hsp90, which interacts
with the P1 region of Tau, is more effective than individual
peptide sequences from the chaperone HSP90 and another
β-hairpin mimic based on Tau sequences. Moreover, β-Hsp90
reduces AD-associated Aβ1-42 aggregation, offering the
development of a dual inhibitor. This work paves the way for
the design of new drugs targeting devastating untreated
amyloid diseases, by mimicking physiological chaperones with
small synthetic peptide drugs.},
keywords = {tau Proteins: metabolism / tau Proteins: chemistry / tau
Proteins: genetics / HSP90 Heat-Shock Proteins: metabolism /
HSP90 Heat-Shock Proteins: chemistry / Humans /
Microtubules: metabolism / Amyloid beta-Peptides: metabolism
/ Alzheimer Disease: metabolism / Protein Aggregation,
Pathological: metabolism / Peptide Fragments: metabolism /
Protein Binding / Protein Aggregates: drug effects / Animals
/ Phosphorylation / Molecular Chaperones: metabolism /
Peptidomimetics: pharmacology / Peptidomimetics: chemistry /
tau Proteins (NLM Chemicals) / HSP90 Heat-Shock Proteins
(NLM Chemicals) / Amyloid beta-Peptides (NLM Chemicals) /
Peptide Fragments (NLM Chemicals) / Protein Aggregates (NLM
Chemicals) / amyloid beta-protein (1-42) (NLM Chemicals) /
Molecular Chaperones (NLM Chemicals) / Peptidomimetics (NLM
Chemicals)},
cin = {AG Zweckstetter},
ddc = {500},
cid = {I:(DE-2719)1410001},
pnm = {352 - Disease Mechanisms (POF4-352)},
pid = {G:(DE-HGF)POF4-352},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:41034231},
pmc = {pmc:PMC12489099},
doi = {10.1038/s41467-025-63824-1},
url = {https://pub.dzne.de/record/281530},
}