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@ARTICLE{Stahl:263808,
author = {Stahl, Fabian and Schmitt, Ina and Denner, Philip and de
Boni, Laura and Wüllner, Ullrich and Breuer, Peter},
title = {{H}igh throughput compound screening in neuronal cells
identifies statins as activators of ataxin 3 expression.},
journal = {Scientific reports},
volume = {13},
number = {1},
issn = {2045-2322},
address = {[London]},
publisher = {Macmillan Publishers Limited, part of Springer Nature},
reportid = {DZNE-2023-00893},
pages = {14911},
year = {2023},
abstract = {The spinocerebellar ataxias (SCA) comprise a group of
inherited neurodegenerative diseases. SCA3 is the most
common form, caused by the expansion of CAG repeats within
the ataxin 3 (ATXN3) gene. The mutation results in the
expression of an abnormal protein, containing long
polyglutamine (polyQ) stretches. The polyQ stretch confers a
toxic gain of function and leads to misfolding and
aggregation of ATXN3 in neurons. Thus, modulators of ATXN3
expression could potentially ameliorate the pathology in
SCA3 patients. Therefore, we generated a CRISPR/Cas9
modified ATXN3-Exon4-Luciferase (ATXN3-LUC) genomic fusion-
and control cell lines to perform a reporter cell line-based
high-throughput screen comprising 2640 bioactive compounds,
including the FDA approved drugs. We found no unequivocal
inhibitors of, but identified statins as activators of the
LUC signal in the ATXN3-LUC screening cell line. We further
confirmed that Simvastatin treatment of wild type SK-N-SH
cells increases ATXN3 mRNA and protein levels which likely
results from direct binding of the activated sterol
regulatory element binding protein 1 (SREBP1) to the ATXN3
promotor. Finally, we observed an increase of normal and
expanded ATXN3 protein levels in a patient-derived cell line
upon Simvastatin treatment, underscoring the potential
medical relevance of our findings.},
keywords = {Humans / Ataxin-3: genetics / Hydroxymethylglutaryl-CoA
Reductase Inhibitors: pharmacology / Neurons / Simvastatin /
Spinocerebellar Ataxias / Ataxin-3 (NLM Chemicals) /
Hydroxymethylglutaryl-CoA Reductase Inhibitors (NLM
Chemicals) / Simvastatin (NLM Chemicals)},
cin = {AG Wüllner / LAT},
ddc = {600},
cid = {I:(DE-2719)1011302 / I:(DE-2719)1040190},
pnm = {353 - Clinical and Health Care Research (POF4-353)},
pid = {G:(DE-HGF)POF4-353},
experiment = {EXP:(DE-2719)LAT-20190308},
typ = {PUB:(DE-HGF)16},
pmc = {pmc:PMC10492798},
pubmed = {pmid:37689718},
doi = {10.1038/s41598-023-41192-4},
url = {https://pub.dzne.de/record/263808},
}