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@ARTICLE{Cameron:284762,
author = {D. P. Cameron and J. Grosser and S. Ladigan and V. Kuzin
and E. Iliopoulou and A. Wiegard and H. Benredjem and K.
Jackson and S.-T. Liffers$^*$ and S. Lueong$^*$ and P. F.
Cheung$^*$ and D. Vangala and M. Pohl and R. Viebahn and C.
Teschendorf and H. Wolters and S. Usta and K. Geng and C.
Kutter and M. Arsenian-Henriksson and J. Siveke$^*$ and A.
Tannapfel and W. Schmiegel and S. A. Hahn and L. Baranello},
title = {{C}oinhibition of topoisomerase 1 and {BRD}4-mediated pause
release selectively kills pancreatic cancer via readthrough
transcription.},
journal = {Science advances},
volume = {9},
number = {41},
issn = {2375-2548},
address = {Washington, DC [u.a.]},
publisher = {Assoc.},
reportid = {DKFZ-2023-02073},
pages = {eadg5109},
year = {2023},
abstract = {Pancreatic carcinoma lacks effective therapeutic strategies
resulting in poor prognosis. Transcriptional dysregulation
due to alterations in KRAS and MYC affects initiation,
development, and survival of this tumor type. Using
patient-derived xenografts of KRAS- and MYC-driven
pancreatic carcinoma, we show that coinhibition of
topoisomerase 1 (TOP1) and bromodomain-containing protein 4
(BRD4) synergistically induces tumor regression by targeting
promoter pause release. Comparing the nascent transcriptome
with the recruitment of elongation and termination factors,
we found that coinhibition of TOP1 and BRD4 disrupts
recruitment of transcription termination factors. Thus, RNA
polymerases transcribe downstream of genes for hundreds of
kilobases leading to readthrough transcription. This occurs
during replication, perturbing replisome progression and
inducing DNA damage. The synergistic effect of TOP1 + BRD4
inhibition is specific to cancer cells leaving normal cells
unaffected, highlighting the tumor's vulnerability to
transcriptional defects. This preclinical study provides a
mechanistic understanding of the benefit of combining TOP1
and BRD4 inhibitors to treat pancreatic carcinomas addicted
to oncogenic drivers of transcription and replication.},
cin = {ED01},
ddc = {500},
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:37831776},
pmc = {pmc:PMC10575591},
doi = {10.1126/sciadv.adg5109},
url = {https://inrepo02.dkfz.de/record/284762},
}