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@ARTICLE{Koch:155320,
author = {Koch, Marilin Sophia and Czemmel, Stefan and Lennartz,
Felix and Beyeler, Sarah and Rajaraman, Srinath and
Przystal, Justyna Magdalena and Govindarajan, Parameswari
and Canjuga, Denis and Neumann, Manfred and Rizzu, Patrizia
and Zwirner, Stefan and Hoetker, Michael Stefan and Zender,
Lars and Walter, Bianca and Tatagiba, Marcos and Raineteau,
Olivier and Heutink, Peter and Nahnsen, Sven and Tabatabai,
Ghazaleh},
title = {{E}xperimental glioma with high b{HLH} expression harbor
increased replicative stress and are sensitive toward {ATR}
inhibition.},
journal = {Neuro-oncology advances},
volume = {2},
number = {1},
issn = {2632-2498},
address = {Oxford},
publisher = {Oxford University Press},
reportid = {DZNE-2021-00587},
pages = {vdaa115},
year = {2020},
note = {ISSN 2632-2498 not unique: **2 hits**.},
abstract = {The overexpression of (basic)helix-loop-helix ((b)HLH)
transcription factors (TFs) is frequent in malignant glioma.
We investigated molecular effects upon disruption of the
(b)HLH network by a dominant-negative variant of the E47
protein (dnE47). Our goal was to identify novel molecular
subgroup-specific therapeutic strategies.Glioma cell lines
LN229, LNZ308, and GS-2/GS-9 were lentivirally transduced.
Functional characterization included immunocytochemistry,
immunoblots, cytotoxic, and clonogenic survival assays in
vitro, and latency until neurological symptoms in vivo.
Results of cap analysis gene expression and RNA-sequencing
were further validated by immunoblot, flow cytometry, and
functional assays in vitro.The induction of dnE47-RFP led to
cytoplasmic sequestration of (b)HLH TFs and antiglioma
activity in vitro and in vivo. Downstream molecular events,
ie, alterations in transcription start site usage and in the
transcriptome revealed enrichment of cancer-relevant
pathways, particularly of the DNA damage response (DDR)
pathway. Pharmacologic validation of this result using
ataxia telangiectasia and Rad3 related (ATR) inhibition led
to a significantly enhanced early and late apoptotic effect
compared with temozolomide alone.Gliomas overexpressing
(b)HLH TFs are sensitive toward inhibition of the ATR
kinase. The combination of ATR inhibition plus temozolomide
or radiation therapy in this molecular subgroup are
warranted.},
keywords = {CAGE (Other) / DDR (Other) / E47 (Other) / RNA-Seq (Other)
/ bHLH transcription factors (Other)},
cin = {AG Rizzu / AG Heutink 1},
ddc = {610},
cid = {I:(DE-2719)1210009 / I:(DE-2719)1210002},
pnm = {345 - Population Studies and Genetics (POF3-345) / 342 -
Disease Mechanisms and Model Systems (POF3-342)},
pid = {G:(DE-HGF)POF3-345 / G:(DE-HGF)POF3-342},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:33134924},
pmc = {pmc:PMC7592426},
doi = {10.1093/noajnl/vdaa115},
url = {https://pub.dzne.de/record/155320},
}