% IMPORTANT: The following is UTF-8 encoded. This means that in the presence
% of non-ASCII characters, it will not work with BibTeX 0.99 or older.
% Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or
% “biber”.
@ARTICLE{Noll:130255,
author = {E. M. Noll$^*$ and C. Eisen$^*$ and A. Stenzinger and E.
Espinet$^*$ and A. Muckenhuber and C. Klein and V. Vogel and
B. Klaus and W. Nadler$^*$ and C. Rösli and C. Lutz and M.
Kulke and J. Engelhardt$^*$ and F. Zickgraf$^*$ and O.
Espinosa$^*$ and M. Schlesner$^*$ and X. Jiang$^*$ and A.
Kopp-Schneider$^*$ and P. Neuhaus and M. Bahra and B. V.
Sinn and R. Eils$^*$ and N. Giese and T. Hackert and O.
Strobel and J. Werner and M. W. Büchler$^*$ and W.
Weichert$^*$ and A. Trumpp$^*$ and M. Sprick$^*$},
title = {{CYP}3{A}5 mediates basal and acquired therapy resistance
in different subtypes of pancreatic ductal adenocarcinoma.},
journal = {Nature medicine},
volume = {22},
number = {3},
issn = {1546-170X},
address = {New York, NY},
publisher = {Nature America Inc.},
reportid = {DKFZ-2017-05335},
pages = {278 - 287},
year = {2016},
abstract = {Although subtypes of pancreatic ductal adenocarcinoma
(PDAC) have been described, this malignancy is clinically
still treated as a single disease. Here we present
patient-derived models representing the full spectrum of
previously identified quasi-mesenchymal (QM-PDA), classical
and exocrine-like PDAC subtypes, and identify two
markers--HNF1A and KRT81--that enable stratification of
tumors into different subtypes by using
immunohistochemistry. Individuals with tumors of these
subtypes showed substantial differences in overall survival,
and their tumors differed in drug sensitivity, with the
exocrine-like subtype being resistant to tyrosine kinase
inhibitors and paclitaxel. Cytochrome P450 3A5 (CYP3A5)
metabolizes these compounds in tumors of the exocrine-like
subtype, and pharmacological or short hairpin RNA
(shRNA)-mediated CYP3A5 inhibition sensitizes tumor cells to
these drugs. Whereas hepatocyte nuclear factor 4, alpha
(HNF4A) controls basal expression of CYP3A5, drug-induced
CYP3A5 upregulation is mediated by the nuclear receptor
NR1I2. CYP3A5 also contributes to acquired drug resistance
in QM-PDA and classical PDAC, and it is highly expressed in
several additional malignancies. These findings designate
CYP3A5 as a predictor of therapy response and as a tumor
cell-autonomous detoxification mechanism that must be
overcome to prevent drug resistance.},
keywords = {Biomarkers, Tumor (NLM Chemicals) / HNF1A protein, human
(NLM Chemicals) / HNF4A protein, human (NLM Chemicals) /
Hepatocyte Nuclear Factor 1-alpha (NLM Chemicals) /
Hepatocyte Nuclear Factor 4 (NLM Chemicals) / KRT81 protein,
human (NLM Chemicals) / Keratins, Hair-Specific (NLM
Chemicals) / Keratins, Type II (NLM Chemicals) / Protein
Kinase Inhibitors (NLM Chemicals) / Receptors, Steroid (NLM
Chemicals) / pregnane X receptor (NLM Chemicals) / Erlotinib
Hydrochloride (NLM Chemicals) / CYP3A5 protein, human (NLM
Chemicals) / Cytochrome P-450 CYP3A (NLM Chemicals) /
Paclitaxel (NLM Chemicals) / Dasatinib (NLM Chemicals)},
cin = {A010 / V960 / B080 / C060 / L101},
ddc = {610},
cid = {I:(DE-He78)A010-20160331 / I:(DE-He78)V960-20160331 /
I:(DE-He78)B080-20160331 / I:(DE-He78)C060-20160331 /
I:(DE-He78)L101-20160331},
pnm = {311 - Signalling pathways, cell and tumor biology
(POF3-311)},
pid = {G:(DE-HGF)POF3-311},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:26855150},
pmc = {pmc:PMC4780258},
doi = {10.1038/nm.4038},
url = {https://inrepo02.dkfz.de/record/130255},
}