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@ARTICLE{Wickstrm:127785,
author = {M. Wickström and C. Dyberg and J. Milosevic and C. Einvik
and R. Calero and B. Sveinbjörnsson and E. Sandén and A.
Darabi and P. Siesjö and M. Kool$^*$ and P. Kogner and N.
Baryawno and J. I. Johnsen},
title = {{W}nt/β-catenin pathway regulates {MGMT} gene expression
in cancer and inhibition of {W}nt signalling prevents
chemoresistance.},
journal = {Nature Communications},
volume = {6},
issn = {2041-1723},
address = {London},
publisher = {Nature Publishing Group},
reportid = {DKFZ-2017-03807},
pages = {8904 -},
year = {2015},
abstract = {The DNA repair enzyme O6-methylguanine-DNA
methyltransferase (MGMT) is commonly overexpressed in
cancers and is implicated in the development of
chemoresistance. The use of drugs inhibiting MGMT has been
hindered by their haematologic toxicity and inefficiency. As
a different strategy to inhibit MGMT we investigated
cellular regulators of MGMT expression in multiple cancers.
Here we show a significant correlation between Wnt
signalling and MGMT expression in cancers with different
origin and confirm the findings by bioinformatic analysis
and immunofluorescence. We demonstrate Wnt-dependent MGMT
gene expression and cellular co-localization between active
β-catenin and MGMT. Pharmacological or genetic inhibition
of Wnt activity downregulates MGMT expression and restores
chemosensitivity of DNA-alkylating drugs in mouse models.
These findings have potential therapeutic implications for
chemoresistant cancers, especially of brain tumours where
the use of temozolomide is frequently used in treatment.},
keywords = {2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide
(NLM Chemicals) / Antineoplastic Agents (NLM Chemicals) /
Benzeneacetamides (NLM Chemicals) / G007-LK (NLM Chemicals)
/ Heterocyclic Compounds, 3-Ring (NLM Chemicals) / LGK974
(NLM Chemicals) / Pyrans (NLM Chemicals) / Pyrazines (NLM
Chemicals) / Pyridines (NLM Chemicals) / Sulfones (NLM
Chemicals) / Triazoles (NLM Chemicals) / Tumor Suppressor
Proteins (NLM Chemicals) / Wnt Proteins (NLM Chemicals) /
XAV939 (NLM Chemicals) / beta Catenin (NLM Chemicals) /
irinotecan (NLM Chemicals) / Vincristine (NLM Chemicals) /
salinomycin (NLM Chemicals) / Dacarbazine (NLM Chemicals) /
Doxorubicin (NLM Chemicals) / DNA Modification Methylases
(NLM Chemicals) / MGMT protein, human (NLM Chemicals) /
Glucose-6-Phosphate Isomerase (NLM Chemicals) / DNA Repair
Enzymes (NLM Chemicals) / Celecoxib (NLM Chemicals) /
Cisplatin (NLM Chemicals) / Camptothecin (NLM Chemicals) /
temozolomide (NLM Chemicals)},
cin = {B062},
ddc = {500},
cid = {I:(DE-He78)B062-20160331},
pnm = {312 - Functional and structural genomics (POF3-312)},
pid = {G:(DE-HGF)POF3-312},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:26603103},
pmc = {pmc:PMC4674781},
doi = {10.1038/ncomms9904},
url = {https://inrepo02.dkfz.de/record/127785},
}