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@ARTICLE{Zhao:300286,
author = {B. Zhao$^*$ and R. Fang$^*$ and H. Schürmann$^*$ and E. J.
Hemmer$^*$ and G. L. Mayer$^*$ and M. Trajkovic-Arsic$^*$
and K. Althoff$^*$ and J. Yang$^*$ and L. Godfrey$^*$ and S.
T. Liffers$^*$ and K. Savvatakis$^*$ and M. Dorsch$^*$ and
B. M. Grüner$^*$ and S. Hahn and M. Remke$^*$ and S. S.
Lueong$^*$ and J. T. Siveke$^*$},
title = {{PLK}1 blockade enhances the anti-tumor effect of {MAPK}
inhibition in pancreatic ductal adenocarcinoma.},
journal = {Cell reports},
volume = {44},
number = {4},
issn = {2211-1247},
address = {Maryland Heights, MO},
publisher = {Cell Press},
reportid = {DKFZ-2025-00739},
pages = {115541},
year = {2025},
abstract = {Despite constitutive Ras/Raf/MAPK pathway activation in
most pancreatic ductal adenocarcinomas (PDACs), treatment
approaches targeting this pathway have primarily been
unsuccessful. We conduct a drug library screen on an MEK
inhibitor (MEKi)-resistant PDAC model and perform
complementary pathway analysis to identify cellular
resistance phenotypes. We use syngeneic models to
investigate the molecular determinants of identified drug
synergism. Our study reveals an enrichment for the hallmarks
of G2/M checkpoints in MEKi-resistant phenotypes from all
investigated models. We find overexpression of Polo-like
kinase 1 (PLK1) and other G2/M checkpoint-related proteins
in MEKi-resistant cells. We identify synergistic activity
between MEK and PLK1 inhibition both in vitro and in vivo
and mechanistically show that dual inhibition of the PLK1
and MEK pathways activates the JNK/c-JUN pathway. This
causes the accumulation of DNA damage, ultimately leading to
apoptotic cell death. Dual PLK1/MEK inhibition emerges as a
promising targeted approach in PDAC.},
keywords = {CP: Cancer (Other) / G1 arrest (Other) / G2/M checkpoint
(Other) / JNK (Other) / KRAS (Other) / MAPK (Other) / MEK
(Other) / PDAC (Other) / PDO (Other) / PLK1 (Other) / cJUN
(Other) / cell cycle (Other) / organoids (Other) / synergism
(Other) / therapy resistance (Other) / trametinib (Other) /
volasertib (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:40188436},
doi = {10.1016/j.celrep.2025.115541},
url = {https://inrepo02.dkfz.de/record/300286},
}