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@ARTICLE{Kalogirou:170397,
author = {C. Kalogirou and J. Linxweiler and P. Schmucker and M. T.
Snaebjornsson$^*$ and W. Schmitz and S. Wach and M. Krebs
and E. Hartmann and M. Puhr and A. Müller and M. Spahn and
A. K. Seitz and T. Frank and H. Marouf and G. Büchel and M.
Eckstein and H. Kübler and M. Eilers and M. Saar and K.
Junker and F. Röhrig and B. Kneitz and M. T. Rosenfeldt and
A. Schulze$^*$},
title = {{M}i{R}-205-driven downregulation of cholesterol
biosynthesis through {SQLE}-inhibition identifies
therapeutic vulnerability in aggressive prostate cancer.},
journal = {Nature Communications},
volume = {12},
number = {1},
issn = {2041-1723},
address = {[London]},
publisher = {Nature Publishing Group UK},
reportid = {DKFZ-2021-01906},
pages = {5066},
year = {2021},
note = {#LA:A410#},
abstract = {Prostate cancer (PCa) shows strong dependence on the
androgen receptor (AR) pathway. Here, we show that squalene
epoxidase (SQLE), an enzyme of the cholesterol biosynthesis
pathway, is overexpressed in advanced PCa and its expression
correlates with poor survival. SQLE expression is controlled
by micro-RNA 205 (miR-205), which is significantly
downregulated in advanced PCa. Restoration of miR-205
expression or competitive inhibition of SQLE led to
inhibition of de novo cholesterol biosynthesis. Furthermore,
SQLE was essential for proliferation of AR-positive PCa cell
lines, including abiraterone or enzalutamide resistant
derivatives, and blocked transactivation of the AR pathway.
Inhibition of SQLE with the FDA approved antifungal drug
terbinafine also efficiently blocked orthotopic tumour
growth in mice. Finally, terbinafine reduced levels of
prostate specific antigen (PSA) in three out of four
late-stage PCa patients. These results highlight SQLE as a
therapeutic target for the treatment of advanced PCa.},
cin = {A410},
ddc = {500},
cid = {I:(DE-He78)A410-20160331},
pnm = {311 - Zellbiologie und Tumorbiologie (POF4-311)},
pid = {G:(DE-HGF)POF4-311},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:34417456},
doi = {10.1038/s41467-021-25325-9},
url = {https://inrepo02.dkfz.de/record/170397},
}