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@ARTICLE{An:292513,
author = {J. An and R. Kurilov$^*$ and T. Peccerella and F. Bergmann
and M. Edderkaoui and A. Lim and X. Zhou and K. Pfütze$^*$
and A. Schulz$^*$ and S. Wolf$^*$ and K. Hu and C.
Springfeld and S. S. Mughal$^*$ and L. Zezlina$^*$ and F.
Fortunato and G. Beyer and J. Mayerle and S. Roth and J.
Hulkkonen and D. Merz and S. Ei and A. Mehrabi and M. Loos
and M. Al-Saeedi and C. W. Michalski and M. W. Büchler and
T. Hackert and B. Brors$^*$ and S. J. Pandol and P.
Bailey$^*$ and J. P. Neoptolemos},
title = {{M}etavert synergises with standard cytotoxics in human
{PDAC} organoids and is associated with transcriptomic
signatures of therapeutic response.},
journal = {Translational oncology},
volume = {49},
issn = {1944-7124},
address = {Ann Arbor, Mich.},
publisher = {[Verlag nicht ermittelbar]},
reportid = {DKFZ-2024-01759},
pages = {102109},
year = {2024},
note = {#EA:B330#LA:B330# / Sample Processing Laborator Pfütze},
abstract = {Despite some recent advances, pancreatic ductal
adenocarcinoma (PDAC) remains a growing oncological
challenge. New drugs capable of targeting more than one
oncogenic pathway may be one way to improve patient
outcomes. This study characterizes the effectiveness of
Metavert a first-in-class dual inhibitor of GSK3-β and
histone deacetylase in treating PDAC as a single agent or in
combination with standard cytotoxics.Thirty-six
Patient-Derived Organoids (hPDOs) characterised by RNASeq
and whole exome sequencing were treated with Metavert alone
or in combination with standard cytotoxics. Transcriptomic
signatures (TS) representing sensitivity to Metavert alone
or sensitivity to Metavert + irinotecan (IR) were evaluated
in 47 patient samples, chemo-naïve in 26 and
post-chemotherapy in 21 (gemcitabine=5; FOLFIRINOX=14,
both=2) with companion multiplexed immunofluorescence and
RNASeq data.Metavert combined with gemcitabine, irinotecan,
5FU, oxaliplatin, and paclitaxel was synergistic in the
hPDOs. Basal-subtype hPDOs were more sensitive to Metavert
alone whereas the Metavert+IR combination exhibited synergy
in Classical-subtype hPDOs with increased apoptosis and
autophagy. hPDO-derived TS evaluated in PDAC tissues
demonstrated that Metavert-TSHi samples were enriched for
mRNA splicing and DNA repair processes; they were associated
with Basal-like tissues but also with GATA6+ve-chemo-naïve
samples and were higher following gemcitabine but not
FOLFIRINOX treatment. In contrast, Metavert+IR-TSHI samples
were enriched for TP53 pathways; they were associated with
Classical-like pretreatment samples and with
GATA6+ve/KRT17+ve hybrid cell types following FOLFIRINOX,
but not gemcitabine treatment, and were unrelated to
transcriptional subtypes.Metavert as a single agent and in
combination with irinotecan offers novel strategies for
treating pancreatic cancer.},
keywords = {Apoptosis (Other) / Autophagy (Other) / GSK3-β (Other) /
Histone deacetylases (Other) / Molecular subtypes (Other) /
Pancreatic cancer (Other)},
cin = {B330 / W190 / HD01},
ddc = {610},
cid = {I:(DE-He78)B330-20160331 / I:(DE-He78)W190-20160331 /
I:(DE-He78)HD01-20160331},
pnm = {312 - Funktionelle und strukturelle Genomforschung
(POF4-312)},
pid = {G:(DE-HGF)POF4-312},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:39217851},
doi = {10.1016/j.tranon.2024.102109},
url = {https://inrepo02.dkfz.de/record/292513},
}