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@ARTICLE{SuryoRahmanto:130382,
author = {A. Suryo Rahmanto and V. Savov and A. Brunner and S. Bolin
and H. Weishaupt and A. Malyukova and G. Rosén and M.
Čančer and S. Hutter$^*$ and A. Sundström and D.
Kawauchi$^*$ and D. Jones$^*$ and C. Spruck and M. D. Taylor
and Y.-J. Cho and S. Pfister$^*$ and M. Kool$^*$ and A.
Korshunov$^*$ and F. J. Swartling and O. Sangfelt},
title = {{FBW}7 suppression leads to {SOX}9 stabilization and
increased malignancy in medulloblastoma.},
journal = {The EMBO journal},
volume = {35},
number = {20},
issn = {1460-2075},
address = {Heidelberg},
publisher = {EMBO Press},
reportid = {DKFZ-2017-05461},
pages = {2192 - 2212},
year = {2016},
abstract = {SOX9 is a master transcription factor that regulates
development and stem cell programs. However, its potential
oncogenic activity and regulatory mechanisms that control
SOX9 protein stability are poorly understood. Here, we show
that SOX9 is a substrate of FBW7, a tumor suppressor, and a
SCF (SKP1/CUL1/F-box)-type ubiquitin ligase. FBW7 recognizes
a conserved degron surrounding threonine 236 (T236) in SOX9
that is phosphorylated by GSK3 kinase and consequently
degraded by SCF(FBW)(7α) Failure to degrade SOX9 promotes
migration, metastasis, and treatment resistance in
medulloblastoma, one of the most common childhood brain
tumors. FBW7 is either mutated or downregulated in
medulloblastoma, and in cases where FBW7 mRNA levels are
low, SOX9 protein is significantly elevated and this
phenotype is associated with metastasis at diagnosis and
poor patient outcome. Transcriptional profiling of
medulloblastoma cells expressing a degradation-resistant
SOX9 mutant reveals activation of pro-metastatic genes and
genes linked to cisplatin resistance. Finally, we show that
pharmacological inhibition of PI3K/AKT/mTOR pathway activity
destabilizes SOX9 in a GSK3/FBW7-dependent manner, rendering
medulloblastoma cells sensitive to cytostatic treatment.},
keywords = {4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo(2,3-d)pyrimidin-4-yl)piperidine-4-carboxamide
(NLM Chemicals) / AZD2014 (NLM Chemicals) / AZD8186 (NLM
Chemicals) / Aniline Compounds (NLM Chemicals) / Cell Cycle
Proteins (NLM Chemicals) / Chromones (NLM Chemicals) / F-Box
Proteins (NLM Chemicals) / Morpholines (NLM Chemicals) /
Protein Kinase Inhibitors (NLM Chemicals) / Pyrimidines (NLM
Chemicals) / Pyrroles (NLM Chemicals) / SOX9 Transcription
Factor (NLM Chemicals) / SOX9 protein, human (NLM Chemicals)
/ Ubiquitin-Protein Ligases (NLM Chemicals) /
Phosphatidylinositol 3-Kinases (NLM Chemicals) / MTOR
protein, human (NLM Chemicals) / TOR Serine-Threonine
Kinases (NLM Chemicals) / Proto-Oncogene Proteins c-akt (NLM
Chemicals) / Glycogen Synthase Kinase 3 (NLM Chemicals) /
FBXW7 protein, human (NLM Chemicals) / Cisplatin (NLM
Chemicals)},
cin = {B062 / G380 / L101},
ddc = {570},
cid = {I:(DE-He78)B062-20160331 / I:(DE-He78)G380-20160331 /
I:(DE-He78)L101-20160331},
pnm = {312 - Functional and structural genomics (POF3-312)},
pid = {G:(DE-HGF)POF3-312},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:27625374},
pmc = {pmc:PMC5069553},
doi = {10.15252/embj.201693889},
url = {https://inrepo02.dkfz.de/record/130382},
}