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@ARTICLE{Schramm:143817,
author = {K. Schramm$^*$ and M. Iskar$^*$ and B. Statz$^*$ and N.
Jäger$^*$ and D. Haag$^*$ and M. Słabicki$^*$ and S. M.
Pfister$^*$ and M. Zapatka$^*$ and J. Gronych$^*$ and D. T.
W. Jones$^*$ and P. Lichter$^*$},
title = {{DECIPHER} pooled sh{RNA} library screen identifies
{PP}2{A} and {FGFR} signaling as potential therapeutic
targets for {DIPG}s.},
journal = {Neuro-Oncology},
volume = {21},
number = {7},
issn = {1523-5866},
address = {Oxford},
publisher = {Oxford Univ. Press},
reportid = {DKFZ-2019-01379},
pages = {867-877},
year = {2019},
abstract = {Diffuse intrinsic pontine gliomas (DIPGs) are highly
aggressive pediatric brain tumors that are characterized by
a recurrent mutation (K27M) within the histone H3 encoding
genes H3F3A or HIST1H3A/B/C. These mutations have been shown
to induce a global reduction in the repressive histone
modification H3K27me3, which together with widespread
changes in DNA methylation patterns results in an extensive
transcriptional reprogramming hampering the identification
of single therapeutic targets based on a molecular
rationale.We applied a large-scale gene knockdown approach
using a pooled shRNA library in combination with
next-generation sequencing in order to identify
DIPG-specific vulnerabilities. The therapeutic potential of
specific inhibitors of candidate targets was validated in a
secondary drug screen.We identified fibroblast growth factor
receptor (FGFR) signaling and the serine/threonine protein
phosphatase 2A (PP2A) as top depleted hits in
patient-derived DIPG cell cultures and validated their
lethal potential by FGF ligand depletion and genetic
knockdown of the PP2A structural subunit PPP2R1A. Further,
pharmacological inhibition of FGFR and PP2A signaling
through ponatinib and LB-100 treatment, respectively,
exhibited strong tumor-specific anti-proliferative and
apoptotic activity in cultured DIPG cells.Our findings
suggest FGFR and PP2A signaling as potential new therapeutic
targets for the treatment of DIPGs.},
cin = {B060 / B062 / B360},
ddc = {610},
cid = {I:(DE-He78)B060-20160331 / I:(DE-He78)B062-20160331 /
I:(DE-He78)B360-20160331},
pnm = {312 - Functional and structural genomics (POF3-312)},
pid = {G:(DE-HGF)POF3-312},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:30943283},
doi = {10.1093/neuonc/noz057},
url = {https://inrepo02.dkfz.de/record/143817},
}