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@ARTICLE{Berberich:148292,
author = {A. Berberich$^*$ and L.-M. Schmitt$^*$ and S. Pusch$^*$ and
T. Hielscher$^*$ and P. Rübmann$^*$ and N. Hucke$^*$ and P.
Latzer$^*$ and B. Heßling$^*$ and D. Lemke$^*$ and T.
Kessler$^*$ and M. Platten$^*$ and W. Wick$^*$},
title = {c{M}yc and {ERK} activity are associated with resistance to
{ALK} inhibitory treatment in glioblastoma.},
journal = {Journal of neuro-oncology},
volume = {146},
number = {1},
issn = {1573-7373},
address = {Dordrecht [u.a.]},
publisher = {Springer Science + Business Media B.V},
reportid = {DKFZ-2019-02856},
pages = {9-23},
year = {2020},
note = {2020 Jan;146(1):9-23#EA:B320#LA:B320#},
abstract = {Anaplastic lymphoma kinase (ALK) is expressed
$in ~ 60\%$ of glioblastomas and conveys tumorigenic
functions. Therefore, ALK inhibitory strategies with
alectinib are conceivable for patients with glioblastoma.
The aims of this preclinical study were to investigate
efficacy as well as to understand and potentially overcome
primary and acquired resistance mechanisms of alectinib in
glioblastoma.Efficacy of alectinib was analyzed dependent on
ALK expression in different glioblastoma initiating cells
and after lentiviral knockdown of ALK. Alectinib resistant
cells were generated by continuous treatment with increasing
alectinib doses over 3 months. M-RNA, phospho-protein and
protein regulation were analyzed to decipher relevant
pathways associated to treatment or resistance and
specifically inhibited to evaluate rational salvage
therapies.Alectinib reduced clonogenicity and proliferation
and induced apoptosis in ALK expressing glioblastoma
initiating cells, whereas cells without ALK expression or
after ALK depletion via knockdown showed primary resistance
against alectinib. High expression of cMyc and activation of
the ERK1/2 pathway conferred resistance against alectinib in
ALK expressing glioblastoma cells. Pharmacological
inhibition of these pathways by cMyc inhibitor or MEK
inhibitor, trametinib, overcame alectinib resistance and
re-sensitized resistant cells to continued alectinib
treatment. The combination of alectinib with radiotherapy
demonstrated synergistic effects in inhibition of
clonogenicity in non-resistant and alectinib resistant
glioblastoma cells.The data offer rationales for alectinib
treatment in ALK expressing glioblastoma and for the use of
ALK expression status as potential biomarker for alectinib
treatment. In addition, the results propose MEK inhibition
or radiotherapy as reasonable salvage treatments after
acquired alectinib resistance.},
cin = {B320 / B300 / C060 / W120 / D170 / HD01},
ddc = {610},
cid = {I:(DE-He78)B320-20160331 / I:(DE-He78)B300-20160331 /
I:(DE-He78)C060-20160331 / I:(DE-He78)W120-20160331 /
I:(DE-He78)D170-20160331 / I:(DE-He78)HD01-20160331},
pnm = {312 - Functional and structural genomics (POF3-312)},
pid = {G:(DE-HGF)POF3-312},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:31776900},
doi = {10.1007/s11060-019-03348-z},
url = {https://inrepo02.dkfz.de/record/148292},
}