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@ARTICLE{Schlotawa:255144,
author = {Schlotawa, Lars and Tyka, Karolina and Kettwig, Matthias
and Ahrens-Nicklas, Rebecca C and Baud, Matthias and
Berulava, Tea and Brunetti-Pierri, Nicola and Gagne, Alyssa
and Herbst, Zackary M and Maguire, Jean A and Monfregola,
Jlenia and Pena Centeno, Tonatiuh and Radhakrishnan,
Karthikeyan and Schroeder, Sophie and Waxman, Elisa A and
Ballabio, Andrea and Dierks, Thomas and Fischer, Andre and
French, Deborah L and Gelb, Michael H and Gärtner, Jutta},
title = {{D}rug screening identifies tazarotene and bexarotene as
therapeutic agents in multiple sulfatase deficiency.},
journal = {EMBO molecular medicine},
volume = {15},
number = {3},
issn = {1757-4676},
address = {Heidelberg},
publisher = {EMBO Press},
reportid = {DZNE-2023-00263},
pages = {e14837},
year = {2023},
note = {CC BY},
abstract = {Multiple sulfatase deficiency (MSD, MIM #272200) results
from pathogenic variants in the SUMF1 gene that impair
proper function of the formylglycine-generating enzyme
(FGE). FGE is essential for the posttranslational activation
of cellular sulfatases. MSD patients display reduced or
absent sulfatase activities and, as a result, clinical signs
of single sulfatase disorders in a unique combination. Up to
date therapeutic options for MSD are limited and mostly
palliative. We performed a screen of FDA-approved drugs
using immortalized MSD patient fibroblasts. Recovery of
arylsulfatase A activity served as the primary readout.
Subsequent analysis confirmed that treatment of primary MSD
fibroblasts with tazarotene and bexarotene, two retinoids,
led to a correction of MSD pathophysiology. Upon treatment,
sulfatase activities increased in a dose- and time-dependent
manner, reduced glycosaminoglycan content decreased and
lysosomal position and size normalized. Treatment of MSD
patient derived induced pluripotent stem cells (iPSC)
differentiated into neuronal progenitor cells (NPC) resulted
in a positive treatment response. Tazarotene and bexarotene
act to ultimately increase the stability of FGE variants.
The results lay the basis for future research on the
development of a first therapeutic option for MSD patients.},
keywords = {Humans / Multiple Sulfatase Deficiency Disease: diagnosis /
Multiple Sulfatase Deficiency Disease: genetics / Multiple
Sulfatase Deficiency Disease: pathology / Bexarotene / Drug
Evaluation, Preclinical / Sulfatases: genetics /
Oxidoreductases Acting on Sulfur Group Donors / Bexarotene
(NLM Chemicals) / drug screening (Other) /
formylglycine-generating enzyme (Other) / lysosomal disorder
(Other) / retinoids (Other) / sulfatase-modifying factor 1
(Other) / tazarotene (NLM Chemicals) / Sulfatases (NLM
Chemicals) / SUMF1 protein, human (NLM Chemicals) /
Oxidoreductases Acting on Sulfur Group Donors (NLM
Chemicals)},
cin = {AG Fischer / Bioinformatics and Genome Dynamics Core},
ddc = {610},
cid = {I:(DE-2719)1410002 / I:(DE-2719)1440016},
pnm = {352 - Disease Mechanisms (POF4-352)},
pid = {G:(DE-HGF)POF4-352},
typ = {PUB:(DE-HGF)16},
pmc = {pmc:PMC9994482},
pubmed = {pmid:36789546},
doi = {10.15252/emmm.202114837},
url = {https://pub.dzne.de/record/255144},
}