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@ARTICLE{Ashry:277877,
author = {R. Ashry and A. M. Mustafa and K. Hausmann and M.
Linnebacher and S. Strand and W. Sippl and M. Wirth$^*$ and
O. H. Krämer},
title = {{NOXA} {A}ccentuates {A}poptosis {I}nduction by a {N}ovel
{H}istone {D}eacetylase {I}nhibitor.},
journal = {Cancers},
volume = {15},
number = {14},
issn = {2072-6694},
address = {Basel},
publisher = {MDPI},
reportid = {DKFZ-2023-01545},
pages = {3650},
year = {2023},
abstract = {Epigenetic modifiers of the histone deacetylase (HDAC)
family are often dysregulated in cancer cells. Experiments
with small molecule HDAC inhibitors (HDACi) have proven that
HDACs are a vulnerability of transformed cells. We evaluated
a novel hydroxamic acid-based HDACi (KH16; termed yanostat)
in human pancreatic ductal adenocarcinoma (PDAC) cells,
short- and long-term cultured colorectal cancer (CRC) cells,
and retinal pigment epithelial cells. We show that KH16
induces cell cycle arrest and apoptosis, both time and dose
dependently in PDAC and CRC cells. This is associated with
altered expression of BCL2 family members controlling
intrinsic apoptosis. Recent data illustrate that PDAC cells
frequently have an altered expression of the pro-apoptotic
BH3-only protein NOXA and that HDACi induce an accumulation
of NOXA. Using PDAC cells with a deletion of NOXA by
CRISPR-Cas9, we found that a lack of NOXA delayed apoptosis
induction by KH16. These results suggest that KH16 is a new
chemotype of hydroxamic acid HDACi with superior activity
against solid tumor-derived cells. Thus, KH16 is a scaffold
for future research on compounds with nanomolar activity
against HDACs.},
keywords = {HDAC (Other) / HDACi (Other) / NOXA (Other) / apoptosis
(Other) / colon cancer (Other) / pancreatic cancer (Other)},
cin = {BE01},
ddc = {610},
cid = {I:(DE-He78)BE01-20160331},
pnm = {899 - ohne Topic (POF4-899)},
pid = {G:(DE-HGF)POF4-899},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:37509312},
pmc = {pmc:PMC10377841},
doi = {10.3390/cancers15143650},
url = {https://inrepo02.dkfz.de/record/277877},
}