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@ARTICLE{Fermi:282718,
author = {V. Fermi and R. Warta and A. Wöllner and C. Lotsch and L.
Jassowicz$^*$ and C. Rapp and M. Knoll$^*$ and G. Jungwirth
and C. Jungk and P. Dao Trong and A. von Deimling$^*$ and A.
Abdollahi$^*$ and A. Unterberg and C. Herold-Mende},
title = {{E}ffective reprogramming of patient-derived {M}2-polarized
glioblastoma-associated microglia/macrophages by treatment
with {GW}2580.},
journal = {Clinical cancer research},
volume = {29},
number = {22},
issn = {1078-0432},
address = {Philadelphia, Pa. [u.a.]},
publisher = {AACR},
reportid = {DKFZ-2023-01844},
pages = {4685-4697},
year = {2023},
note = {2023 Nov 14;29(22):4685-4697},
abstract = {Targeting immunosuppressive and pro-tumorigenic
glioblastoma-associated macrophages and microglial cells
(GAMs) has great potential to improve patient outcomes.
Colony stimulating factor-1 receptor (CSF1R) has emerged as
a promising target for reprograming anti-inflammatory
M2-like GAMs. However, treatment data on patient-derived,
tumor-educated GAMs and their influence on the adaptive
immunity are lacking.CD11b+-GAMs freshly isolated from
patient tumors were treated with CSF1R-targeting drugs
PLX3397, BLZ945, and GW2580. Phenotypical changes upon
treatment were assessed using RNAseq, flow cytometry, and
cytokine quantification. Functional analyses included iNOS
activity, phagocytosis, transmigration, and autologous tumor
cell killing assays. Antitumor effects and changes in GAM
activation were confirmed in a complex patient-derived 3D
tumor organoid model serving as a tumor avatar.The most
effective reprogramming of GAMs was observed upon GW2580
treatment, which led to the downregulation of M2-related
markers, IL-6, and IL-10, ERK1/2 and MAPK signaling
pathways, while M1-like markers, gene set enrichment
indicating activated MHC-II presentation, phagocytosis, and
T-cell killing were substantially increased. Moreover,
treatment of patient-derived glioblastoma organoids with
GW2580 confirmed successful reprogramming, resulting in
impaired tumor cell proliferation. In line with its failure
in clinical trials, PLX3397 was ineffective in our
analysis.This comparative analysis of CSF1R-targeting drugs
on patient-derived GAMs and human glioblastoma avatars
identified GW2580 as the most powerful inhibitor with the
ability to polarize immunosuppressive GAMs to a
proinflammatory phenotype, supporting antitumor T cell
responses while also exerting a direct antitumor effect.
These data indicate that GW2580 could be an important pillar
in future therapies for glioblastoma.},
cin = {B060 / E210 / B300 / HD01},
ddc = {610},
cid = {I:(DE-He78)B060-20160331 / I:(DE-He78)E210-20160331 /
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:37682326},
doi = {10.1158/1078-0432.CCR-23-0576},
url = {https://inrepo02.dkfz.de/record/282718},
}