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@ARTICLE{Koch:877590,
author = {Koch, Katharina and Hartmann, Rudolf and Tsiampali, Julia
and Uhlmann, Constanze and Nickel, Ann-Christin and He,
Xiaoling and Kamp, Marcel A. and Sabel, Michael and Barker,
Roger A. and Steiger, Hans-Jakob and Hänggi, Daniel and
Willbold, Dieter and Maciaczyk, Jaroslaw and Kahlert, Ulf
D.},
title = {{A} comparative pharmaco-metabolomic study of glutaminase
inhibitors in glioma stem-like cells confirms biological
effectiveness but reveals differences in target-specificity},
journal = {Cell death discovery},
volume = {6},
number = {1},
issn = {2058-7716},
address = {London},
publisher = {Nature Publishing Group816700},
reportid = {FZJ-2020-02312},
pages = {20},
year = {2020},
abstract = {Cancer cells upregulate anabolic processes to maintain high
rates of cellular turnover. Limiting the supply
ofmacromolecular precursors by targeting enzymes involved in
biosynthesis is a promising strategy in cancer
therapy.Several tumors excessively metabolize glutamine to
generate precursors for nonessential amino acids,
nucleotides,and lipids, in a process called glutaminolysis.
Here we show that pharmacological inhibition of glutaminase
(GLS)eradicates glioblastoma stem-like cells (GSCs), a small
cell subpopulation in glioblastoma (GBM) responsible for
therapyresistance and tumor recurrence. Treatment with small
molecule inhibitors compound 968 and CB839
effectivelydiminished cell growth and in vitro clonogenicity
of GSC neurosphere cultures. However, our
pharmaco-metabolicstudies revealed that only CB839 inhibited
GLS enzymatic activity thereby limiting the influx of
glutamine derivatesinto the TCA cycle. Nevertheless, the
effects of both inhibitors were highly GLS specific, since
treatment sensitivitymarkedly correlated with GLS protein
expression. Strikingly, we found GLS overexpressed in in
vitro GSC models ascompared with neural stem cells (NSC).
Moreover, our study demonstrates the usefulness of in vitro
pharmaco-metabolomics to score target specificity of
compounds thereby refining drug development and risk
assessment.},
cin = {IBI-7},
ddc = {610},
cid = {I:(DE-Juel1)IBI-7-20200312},
pnm = {552 - Engineering Cell Function (POF3-552)},
pid = {G:(DE-HGF)POF3-552},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:32337072},
UT = {WOS:000526352700001},
doi = {10.1038/s41420-020-0258-3},
url = {https://juser.fz-juelich.de/record/877590},
}