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@ARTICLE{Switzeny:302291,
author = {O. Switzeny and S. Pusch$^*$ and M. Christmann and B.
Kaina},
title = {{IDH}1 {M}utation {I}mpacts {DNA} {R}epair {T}hrough
{ALKBH}2 {R}endering {G}lioblastoma {C}ells {S}ensitive to
{A}rtesunate.},
journal = {Biomedicines},
volume = {13},
number = {6},
issn = {2227-9059},
address = {Basel},
publisher = {MDPI},
reportid = {DKFZ-2025-01310},
pages = {1479},
year = {2025},
abstract = {Background: Isocitrate dehydrogenase 1 and 2 (IDH1 and
IDH2) are enzymes that catalyze the oxidative
decarboxylation of isocitrate to alpha-ketoglutarate
(α-KG), which is essential for many metabolic processes,
including some steps in DNA repair. In tumors, notably in
gliomas, IDH1 and IDH2 are frequently mutated. The mutation
found in different cancers is functionally active, causing,
instead of α-KG, the formation of 2-hydroxyglutarate
(2-HG), which inhibits α-KG-dependent enzymes. Gliomas
harboring mutated IDH1/2 show a better prognosis than IDH1
wild-type (wt) tumors of the same grade, which might result
from the inhibition of DNA repair functions. A DNA repair
enzyme dependent on α-KG is alkB homolog 2 (ALKBH2), which
removes several lesions from DNA. These findings prompted us
to investigate the response of glioma cells to artesunate
(ART), a plant ingredient with genotoxic and anticancer
activity currently used in several trials. Materials and
Methods: We used isogenic glioblastoma cell lines that
express IDH1 wild-type or, based on a TET-inducible system,
the IDH1 mutant (mt) protein, and treated them with
increasing doses of artesunate. We also treated glioblastoma
cells with 2-HG, generated ALKBH2 knockout cells, and
checked their sensitivity to the cytotoxic effects of
artesunate. Results: We show that the cell-killing effect of
ART is enhanced if the IDH1 mutant (R132H) is expressed in
glioblastoma cells. Further, we show that 2-HG imitates the
effect of IDH1mt as 2-HG ameliorates the cytotoxicity of
ART. Finally, we demonstrate that the knockout of ALKBH2
causes the sensitization of glioblastoma cells to ART.
Conclusions: The data indicate that ALKBH2 protects against
the anticancer effect of ART, and the mutation of IDH1/2
commonly occurring in low-grade gliomas sensitizes to ART
via an ALKBH2-dependent mechanism. The data support the use
of ART in the therapy of IDH1/2-mutated cancers both in
combination with chemotherapy and adjuvant treatment.},
keywords = {ALKBH2 (Other) / DNA repair (Other) / IDH1 (Other) /
artesunate (Other) / glioblastoma (Other) / temozolomide
(Other)},
cin = {B300 / HD01},
ddc = {570},
cid = {I:(DE-He78)B300-20160331 / I:(DE-He78)HD01-20160331},
pnm = {312 - Funktionelle und strukturelle Genomforschung
(POF4-312)},
pid = {G:(DE-HGF)POF4-312},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:40564198},
doi = {10.3390/biomedicines13061479},
url = {https://inrepo02.dkfz.de/record/302291},
}