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@ARTICLE{Pohly:298340,
author = {M. F. Pohly and K. Putzker$^*$ and S. Scheinost and L. Ben
Taarit and T. Walther$^*$ and S. Kummer and T. Wertheimer
and M. Lin and T. H. L. Do and K. Handler and J. Michler and
J. Kivioja and K. Bach and S. Kisele and J. Kim and S.
Dietrich and B. Bornhauser and W. W. Wong and B. Becher and
A. Moor and J. D. Lewis and X. M. Ficht and J. Lu and W.
Huber and T. Zenz},
title = {{IAP} dependency of {T}-cell prolymphocytic leukemia
identified by high-throughput drug screening.},
journal = {Blood},
volume = {145},
number = {20},
issn = {0006-4971},
address = {Washington, DC},
publisher = {American Society of Hematology},
reportid = {DKFZ-2025-00244},
pages = {2336-2352},
year = {2025},
note = {2025 May 15;145(20):2336-2352},
abstract = {T-cell prolymphocytic leukemia (T-PLL) is an aggressive
lymphoid malignancy with limited treatment options. To
discover new treatment targets for T-PLL, we performed
high-throughput drug sensitivity screening on 30 primary
patient samples ex-vivo. After screening over 2'800 unique
compounds, we found T-PLL to be more resistant to most drug
classes, including chemotherapeutics, compared to other
blood cancers. Furthermore, we discovered previously not
reported vulnerabilities of T-PLL. T-PLL cells exhibited a
particular sensitivity to drugs targeting autophagy
(thapsigargin, bafilomycin A1), nuclear export (selinexor),
and inhibitor of apoptosis proteins (IAPs) (birinapant),
sensitivities that were also shared by other T-cell
malignancies. Through bulk and single-cell RNA-Sequencing we
found these compounds to activate the toll-like-receptor
(TLR) (bafilomycin A1), p53 (selinexor), and TNF-ɑ/NFκB
signaling pathways (birinapant) in T-PLL cells. Focussing on
birinapant for its potential in drug repurposing, we
uncovered that IAP inhibitor-induced cell death was
primarily necroptotic and dependent on TNF-ɑ. Through
spectral flow cytometry we confirmed the absence of cleaved
caspase-3 in IAP inhibitor treated T-PLL cells and show that
IAP inhibition reduces the proliferation of T-PLL cells
stimulated ex-vivo, while showing only a limited effect on
non-malignant T-cells. In summary, our study maps the drug
sensitivity of T-PLL across a broad range of targets and
identifies new therapeutic approaches for T-PLL by targeting
IAPs, XPO1 and autophagy, highlighting potential candidates
for drug repurposing and novel treatment strategies.},
cin = {W040 / B340},
ddc = {610},
cid = {I:(DE-He78)W040-20160331 / I:(DE-He78)B340-20160331},
pnm = {312 - Funktionelle und strukturelle Genomforschung
(POF4-312)},
pid = {G:(DE-HGF)POF4-312},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:39869826},
doi = {10.1182/blood.2024027171},
url = {https://inrepo02.dkfz.de/record/298340},
}