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@MISC{Mller:279497,
author = {Müller, Stephan A and Lichtenthaler, Stefan},
title = {{D}ataset: {P}harmacoproteomics of non-human primate
cerebrospinal fluid after {BACE} inhibition},
publisher = {PRoteomics IDEntifications Database},
reportid = {DZNE-2025-00824},
year = {2023},
abstract = {The protease BACE1 is a major drug target for Alzheimer’s
disease, but chronic BACE1 inhibition is associated with
non-progressive worsening that may be caused by modulation
of unknown physiological BACE1 substrates. To identify in
vivo-relevant BACE1 substrates we applied pharmacoproteomics
to non-human-primate cerebrospinal fluid (CSF) after acute
treatment with BACE inhibitors. Besides SEZ6, the strongest,
dose-dependent reduction was observed for the
pro-inflammatory cytokine receptor gp130/IL6ST, which we
establish as a new in vivo BACE1 substrate. Gp130 was also
reduced in human CSF from a clinical trial with a BACE
inhibitor and in plasma of BACE1-deficient mice.
Mechanistically, we demonstrate that BACE1 directly cleaves
gp130, thereby attenuating membrane-bound gp130 and
increasing soluble gp130 abundance and controlling gp130
function in neuronal IL-6 signaling and neuronal survival
upon growth-factor withdrawal. In conclusion, BACE1 is a new
modulator of gp130 function. The BACE1-cleaved, soluble
gp130 may serve as a pharmacodynamic BACE1 activity marker
to reduce the occurrence of side effects of chronic BACE1
inhibition in humans.},
cin = {AG Lichtenthaler},
cid = {I:(DE-2719)1110006},
pnm = {352 - Disease Mechanisms (POF4-352)},
pid = {G:(DE-HGF)POF4-352},
typ = {PUB:(DE-HGF)32},
url = {https://pub.dzne.de/record/279497},
}