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@ARTICLE{Carraro:165276,
author = {Carraro, Caterina and Bonaguro, Lorenzo and
Schulte-Schrepping, Jonas and Horne, Arik and Oestreich,
Marie and Warnat-Herresthal, Stefanie and Helbing, Tim and
De Franco, Michele and Händler, Kristian and Mukherjee,
Sach and Ulas, Thomas and Gandin, Valentina and Goettlich,
Richard and Aschenbrenner, Anna Christin and Schultze,
Joachim L and Gatto, Barbara},
title = {{D}ecoding mechanism of action and sensitivity to drug
candidates from integrated transcriptome and chromatin
state.},
journal = {eLife},
volume = {11},
issn = {2050-084X},
address = {Cambridge},
publisher = {eLife Sciences Publications},
reportid = {DZNE-2022-01569},
pages = {e78012},
year = {2022},
note = {CC BY: https://creativecommons.org/licenses/by/4.0/},
abstract = {Omics-based technologies are driving major advances in
precision medicine, but efforts are still required to
consolidate their use in drug discovery. In this work, we
exemplify the use of multi-omics to support the development
of 3-chloropiperidines, a new class of candidate anticancer
agents. Combined analyses of transcriptome and chromatin
accessibility elucidated the mechanisms underlying
sensitivity to test agents. Furthermore, we implemented a
new versatile strategy for the integration of RNA- and
ATAC-seq (Assay for Transposase-Accessible Chromatin) data,
able to accelerate and extend the standalone analyses of
distinct omic layers. This platform guided the construction
of a perturbation-informed basal signature predicting cancer
cell lines' sensitivity and to further direct compound
development against specific tumor types. Overall, this
approach offers a scalable pipeline to support the early
phases of drug discovery, understanding of mechanisms, and
potentially inform the positioning of therapeutics in the
clinic.},
keywords = {Chromatin / Precision Medicine / RNA / Transcriptome /
Transposases: metabolism / chromatin accessibility (Other) /
computational biology (Other) / drug candidate (Other) /
human (Other) / mechanism of action (Other) / multi-omics
(Other) / sensitivity ML prediction (Other) / systems
biology (Other) / transcriptome (Other) / Chromatin (NLM
Chemicals) / RNA (NLM Chemicals) / Transposases (NLM
Chemicals)},
cin = {AG Schultze / $R\&D$ PRECISE / AG Mukherjee},
ddc = {600},
cid = {I:(DE-2719)1013031 / I:(DE-2719)5000031 /
I:(DE-2719)1013030},
pnm = {352 - Disease Mechanisms (POF4-352) / 354 - Disease
Prevention and Healthy Aging (POF4-354)},
pid = {G:(DE-HGF)POF4-352 / G:(DE-HGF)POF4-354},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:36043458},
pmc = {pmc:PMC9433094},
doi = {10.7554/eLife.78012},
url = {https://pub.dzne.de/record/165276},
}