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@ARTICLE{Hornung:277879,
author = {Hornung, Simon and Vogl, Dominik P and Naltsas, Denise and
Volta, Beatrice Dalla and Ballmann, Markus and Marcon,
Beatrice and Syed, Muhammed Muazzam Kamil and Wu, Yiyang and
Spanopoulou, Anna and Feederle, Regina and Heidrich, Luzia
and Bernhagen, Jürgen and Koeglsperger, Thomas and
Höglinger, Günter U and Rammes, Gerhard and Lashuel, Hilal
A and Kapurniotu, Aphrodite},
title = {{M}ulti-{T}argeting {M}acrocyclic {P}eptides as {N}anomolar
{I}nhibitors of {S}elf- and {C}ross-{S}eeded {A}myloid
{S}elf-{A}ssembly of α-{S}ynuclein.},
journal = {Angewandte Chemie / International edition},
volume = {64},
number = {14},
issn = {1433-7851},
address = {Weinheim},
publisher = {Wiley-VCH},
reportid = {DZNE-2025-00499},
pages = {e202422834},
year = {2025},
abstract = {Amyloid self-assembly of α-synuclein (αSyn) is linked to
the pathogenesis of Parkinson's disease (PD). Type 2
diabetes (T2D) has recently emerged as a risk factor for PD.
Cross-interactions between their amyloidogenic proteins may
act as molecular links. In fact, fibrils of islet amyloid
polypeptide (IAPP) (T2D) can cross-seed αSyn
amyloidogenesis and αSyn and IAPP colocalize in PD brains.
Inhibition of both self- and IAPP-cross-seeded αSyn
amyloidogenesis could thus interfere with PD pathogenesis.
Here we show that macrocyclic peptides, designed to mimic
IAPP self-/cross-interaction sites and previously found to
inhibit amyloidogenesis of IAPP and/or Alzheimer's disease
(AD) amyloid-β peptide Aβ40(42), are nanomolar inhibitors
of both self- and IAPP-cross-seeded amyloid self-assembly of
αSyn. Anti-amyloid function is mediated by nanomolar
affinity interactions with αSyn via three αSyn regions
which are identified as key sites of both αSyn
self-assembly and its cross-interactions with IAPP. We also
show that the peptides block Aβ42-mediated cross-seeding of
αSyn as well. Based on their broad spectrum anti-amyloid
function and additional drug-like features, these peptides
are leads for multifunctional anti-amyloid drugs in PD, T2D,
AD, and their comorbidities, while the identified αSyn key
segments are valuable targets for novel, multi-site
targeting amyloid inhibitors in PD and related
synucleinopathies.},
keywords = {alpha-Synuclein: metabolism / alpha-Synuclein: chemistry /
alpha-Synuclein: antagonists $\&$ inhibitors / Humans /
Amyloid: metabolism / Amyloid: antagonists $\&$ inhibitors /
Amyloid: chemistry / Islet Amyloid Polypeptide: metabolism /
Islet Amyloid Polypeptide: chemistry / Amyloid
beta-Peptides: metabolism / Amyloid beta-Peptides: chemistry
/ Amyloid beta-Peptides: antagonists $\&$ inhibitors /
Macrocyclic Compounds: chemistry / Macrocyclic Compounds:
pharmacology / Peptides: chemistry / Peptides: pharmacology
/ (cross-)seeding (Other) / amyloid inhibitor (Other) /
protein-protein interactions (Other) / self-assembly (Other)
/ α-synuclein (Other) / alpha-Synuclein (NLM Chemicals) /
Amyloid (NLM Chemicals) / Islet Amyloid Polypeptide (NLM
Chemicals) / Amyloid beta-Peptides (NLM Chemicals) /
Macrocyclic Compounds (NLM Chemicals) / Peptides (NLM
Chemicals)},
cin = {AG Herms / AG Feederle / Clinical Research (Munich)},
ddc = {540},
cid = {I:(DE-2719)1110001 / I:(DE-2719)1140004 /
I:(DE-2719)1111015},
pnm = {352 - Disease Mechanisms (POF4-352) / 353 - Clinical and
Health Care Research (POF4-353)},
pid = {G:(DE-HGF)POF4-352 / G:(DE-HGF)POF4-353},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:39822034},
doi = {10.1002/anie.202422834},
url = {https://pub.dzne.de/record/277879},
}