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@ARTICLE{Shimshek:138397,
author = {Shimshek, Derya R and Jacobson, Laura H and Kolly, Carine
and Zamurovic, Natasa and Balavenkatraman, Kamal Kumar and
Morawiec, Laurent and Kreutzer, Robert and Schelle, Juliane
and Jucker, Mathias and Bertschi, Barbara and Theil,
Diethilde and Heier, Annabelle and Bigot, Karine and Beltz,
Karen and Machauer, Rainer and Brzak, Irena and Perrot,
Ludovic and Neumann, Ulf},
title = {{P}harmacological {BACE}1 and {BACE}2 inhibition induces
hair depigmentation by inhibiting {PMEL}17 processing in
mice.},
journal = {Scientific reports},
volume = {6},
number = {1},
issn = {2045-2322},
address = {[London]},
publisher = {Macmillan Publishers Limited, part of Springer Nature},
reportid = {DZNE-2020-04719},
pages = {21917},
year = {2016},
abstract = {Melanocytes of the hair follicle produce melanin and are
essential in determining the differences in hair color.
Pigment cell-specific MELanocyte Protein (PMEL17) plays a
crucial role in melanogenesis. One of the critical steps is
the amyloid-like functional oligomerization of PMEL17. Beta
Site APP Cleaving Enzyme-2 (BACE2) and γ-secretase have
been shown to be key players in generating the proteolytic
fragments of PMEL17. The β-secretase (BACE1) is responsible
for the generation of amyloid-β (Aβ) fragments in the
brain and is therefore proposed as a therapeutic target for
Alzheimer's disease (AD). Currently BACE1 inhibitors, most
of which lack selectivity over BACE2, have demonstrated
efficacious reduction of amyloid-β peptides in animals and
the CSF of humans. BACE2 knock-out mice have a deficiency in
PMEL17 proteolytic processing leading to impaired melanin
storage and hair depigmentation. Here, we confirm
BACE2-mediated inhibition of PMEL17 proteolytic processing
in vitro in mouse and human melanocytes. Furthermore, we
show that wildtype as well as bace2(+/-) and bace2(-/-) mice
treated with a potent dual BACE1/BACE2 inhibitor NB-360
display dose-dependent appearance of irreversibly
depigmented hair. Retinal pigmented epithelium showed no
morphological changes. Our data demonstrates that BACE2 as
well as additional BACE1 inhibition affects melanosome
maturation and induces hair depigmentation in mice.},
keywords = {Amyloid Precursor Protein Secretases: antagonists $\&$
inhibitors / Amyloid Precursor Protein Secretases: genetics
/ Amyloid Precursor Protein Secretases: metabolism / Amyloid
beta-Peptides: metabolism / Animals / Aspartic Acid
Endopeptidases: antagonists $\&$ inhibitors / Aspartic Acid
Endopeptidases: genetics / Aspartic Acid Endopeptidases:
metabolism / Blotting, Western / Cell Line, Tumor / Female /
Hair: drug effects / Hair: metabolism / Hair: pathology /
Humans / Male / Melanins: metabolism / Melanocytes: cytology
/ Melanocytes: metabolism / Mice / Mice, Inbred C57BL /
Mice, Knockout / Microscopy, Fluorescence / Peptide
Fragments: metabolism / Picolinic Acids: pharmacology /
Pigmentation: drug effects / Prosencephalon: metabolism /
Prosencephalon: pathology / Protease Inhibitors:
pharmacology / RNA, Messenger: metabolism / Real-Time
Polymerase Chain Reaction / Thiazines: pharmacology / Uvea:
drug effects / Uvea: metabolism / Uvea: pathology / gp100
Melanoma Antigen: antagonists $\&$ inhibitors / gp100
Melanoma Antigen: metabolism / Amyloid beta-Peptides (NLM
Chemicals) / Bace2 protein, mouse (NLM Chemicals) / Melanins
(NLM Chemicals) / NB-360 (NLM Chemicals) / Peptide Fragments
(NLM Chemicals) / Picolinic Acids (NLM Chemicals) / Pmel
protein, mouse (NLM Chemicals) / Protease Inhibitors (NLM
Chemicals) / RNA, Messenger (NLM Chemicals) / Thiazines (NLM
Chemicals) / amyloid beta-protein (1-40) (NLM Chemicals) /
gp100 Melanoma Antigen (NLM Chemicals) / Amyloid Precursor
Protein Secretases (NLM Chemicals) / Aspartic Acid
Endopeptidases (NLM Chemicals) / Bace1 protein, mouse (NLM
Chemicals)},
cin = {AG Jucker},
ddc = {600},
cid = {I:(DE-2719)1210001},
pnm = {342 - Disease Mechanisms and Model Systems (POF3-342)},
pid = {G:(DE-HGF)POF3-342},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:26912421},
pmc = {pmc:PMC4766495},
doi = {10.1038/srep21917},
url = {https://pub.dzne.de/record/138397},
}