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@ARTICLE{Kuhn:186734,
author = {C. Kuhn and M. Boeschen and M. Philip$^*$ and T.
Schöneberg and D. Thor and S. Horn$^*$},
title = {{C}andidate drugs associated with sensitivity of cancer
cell lines with {DLST} amplification or high m{RNA} levels.},
journal = {OncoTarget},
volume = {14},
number = {1},
issn = {1949-2553},
address = {[Erscheinungsort nicht ermittelbar]},
publisher = {Impact Journals LLC},
reportid = {DKFZ-2023-00086},
pages = {14-20},
year = {2023},
abstract = {Overexpression of the dihydrolipoamide
S-succinyltransferase (DLST) is associated with poor outcome
in neuroblastoma patients and triple-negative breast cancer
(TNBC) and specifically with the oxidative phosphorylation
(OXPHOS) pathway. Inhibitors of OXPHOS were previously
suggested as a potential therapeutic strategy for a subset
of patients with high-risk neuroblastoma. Here, we tested if
cell lines with DLST amplifications or high mRNA levels were
associated with sensitivity to 250 drugs from the Genomics
of Drug Sensitivity in Cancer (GDSC) dataset by comparing
them to cell lines without these changes. DLST-altered cell
lines were more sensitive to 7 approved drugs, among these
obatoclax mesylate, a BCL2 inhibitor that reduces OXPHOS in
human leukemia stem cells. Moreover, several protein kinase
inhibitors were identified to be efficient in cell lines
with DLST amplifications or high mRNA levels, suggesting a
vulnerability of DLST-altered cell lines for drugs targeting
the ERK/MAPK pathway. Furthermore, increased DLST expression
in cell lines with driver mutations in KRAS supported this
relationship. We therefore conclude that, in addition to
OXPHOS, protein kinases could be potential targets of
therapy in the presence of DLST amplifications or high mRNA
levels. The new drug candidates proposed here could serve in
experimental testing on drug efficacy in knock-in cell lines
and DLST-activated tumors.},
keywords = {DLST (Other) / drug repurposing (Other) / drug resistance
(Other) / drug sensitivity (Other) / neuroblastoma (Other)},
cin = {ED01},
ddc = {610},
cid = {I:(DE-He78)ED01-20160331},
pnm = {899 - ohne Topic (POF4-899)},
pid = {G:(DE-HGF)POF4-899},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:36634214},
doi = {10.18632/oncotarget.28342},
url = {https://inrepo02.dkfz.de/record/186734},
}