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@ARTICLE{Lopez:282878,
author = {V. Lopez and H. J. M. Schuh and S. Mirza and V. J. Vaaßen
and M. S. Schmidt and K. Sylvester and R. M. Idris and C.
Renn and L. Schäkel and J. Pelletier and J. Sévigny and A.
Naggi and B. Scheffler$^*$ and S.-Y. Lee and G. Bendas and
C. E. Müller},
title = {{H}eparins are potent inhibitors of ectonucleotide
pyrophosphatase/phospho-diesterase-1 ({NPP}1) - a promising
target for the immunotherapy of cancer.},
journal = {Frontiers in immunology},
volume = {14},
issn = {1664-3224},
address = {Lausanne},
publisher = {Frontiers Media},
reportid = {DKFZ-2023-01880},
pages = {1173634},
year = {2023},
abstract = {Heparins, naturally occurring glycosaminoglycans, are
widely used for thrombosis prevention. Upon application as
anticoagulants in cancer patients, heparins were found to
possess additional antitumor activities. Ectonucleotidases
have recently been proposed as novel targets for cancer
immunotherapy.In the present study, we discovered that
heparin and its derivatives act as potent, selective,
allosteric inhibitors of the poorly investigated
ectonucleotidase NPP1 (nucleotide
pyrophosphatase/phosphodiesterase-1, CD203a).
Structure-activity relationships indicated that NPP1
inhibition could be separated from the compounds'
antithrombotic effect. Moreover, unfractionated heparin
(UFH) and different low molecular weight heparins (LMWHs)
inhibited extracellular adenosine production by the
NPP1-expressing glioma cell line U87 at therapeutically
relevant concentrations. As a consequence, heparins
inhibited the ability of U87 cell supernatants to induce
CD4+ T cell differentiation into immunosuppressive Treg
cells.NPP1 inhibition likely contributes to the anti-cancer
effects of heparins, and their specific optimization may
lead to improved therapeutics for the immunotherapy of
cancer.},
keywords = {NPP1 (Other) / U87 glioblastoma cells (Other) / adenosine
(Other) / ectonucleotidase inhibitors (Other) / heparin
(Other) / immuno-oncology (Other)},
cin = {ED01},
ddc = {610},
cid = {I:(DE-He78)ED01-20160331},
pnm = {899 - ohne Topic (POF4-899)},
pid = {G:(DE-HGF)POF4-899},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:37711611},
pmc = {pmc:PMC10497752},
doi = {10.3389/fimmu.2023.1173634},
url = {https://inrepo02.dkfz.de/record/282878},
}