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@ARTICLE{Vollmer:284402,
author = {J. Vollmer$^*$ and J. Ecker$^*$ and T. Hielscher$^*$ and G.
Valinciute$^*$ and J. Ridinger$^*$ and N. Jamaladdin$^*$ and
H. Peterziel$^*$ and C. M. van Tilburg$^*$ and I. Oehme$^*$
and O. Witt$^*$ and T. Milde$^*$},
title = {{C}lass {I} {HDAC} inhibition reduces {DNA} damage repair
capacity of {MYC}-amplified medulloblastoma cells.},
journal = {Journal of neuro-oncology},
volume = {164},
number = {3},
issn = {0167-594X},
address = {Dordrecht [u.a.]},
publisher = {Springer Science + Business Media B.V},
reportid = {DKFZ-2023-01991},
pages = {617-632},
year = {2023},
note = {#EA:B310#LA:B310# / 2023 Sep;164(3):617-632},
abstract = {MYC-driven Group 3 medulloblastoma (MB) (subtype II) is a
highly aggressive childhood brain tumor. Sensitivity of
MYC-driven MB to class I histone deacetylase inhibitors
(HDACi) has been previously demonstrated in vitro and in
vivo. In this study we characterize the transcriptional
effects of class I HDACi in MYC-driven MB and explore
beneficial drug combinations.MYC-amplified Group 3 MB cells
(HD-MB03) were treated with class I HDACi entinostat.
Changes in the gene expression profile were quantified on a
microarray. Bioinformatic assessment led to the
identification of pathways affected by entinostat treatment.
Five drugs interfering with these pathways (olaparib,
idasanutlin, ribociclib, selinexor, vinblastine) were tested
for synergy with entinostat in WST-8 metabolic activity
assays in a 5 × 5 combination matrix design. Synergy was
validated in cell count and flow cytometry experiments. The
effect of entinostat and olaparib on DNA damage was
evaluated by γH2A.X quantification in immunoblotting,
fluorescence microscopy and flow cytometry.Entinostat
treatment changed the expression of genes involved in 22
pathways, including downregulation of DNA damage response.
The PARP1 inhibitors olaparib and pamiparib showed synergy
with entinostat selectively in MYC-amplified MB cells,
leading to increased cell death, decreased viability and
increased formation of double strand breaks, as well as
increased sensitivity to additional induction of DNA damage
by doxorubicin. Non-MYC-amplified MB cells and normal human
fibroblasts were not susceptible to this triple
treatment.Our study identifies the combination of entinostat
with olaparib as a new potential therapeutic approach for
MYC-driven Group 3 MB.},
keywords = {DNA-damage (Other) / HDAC (Other) / MYC (Other) /
Medulloblastoma (Other) / Synergy (Other)},
cin = {B310 / HD01 / C060},
ddc = {610},
cid = {I:(DE-He78)B310-20160331 / I:(DE-He78)HD01-20160331 /
I:(DE-He78)C060-20160331},
pnm = {312 - Funktionelle und strukturelle Genomforschung
(POF4-312)},
pid = {G:(DE-HGF)POF4-312},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:37783879},
doi = {10.1007/s11060-023-04445-w},
url = {https://inrepo02.dkfz.de/record/284402},
}