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Published in 2019 at "Neuro-oncology"
DOI: 10.1093/neuonc/noz164
Abstract: BACKGROUND ONC201 is a dopamine receptor D2 (DRD2) antagonist that penetrates the blood-brain barrier. ONC201 efficacy has been shown in glioblastoma animal models and is inversely correlated with dopamine receptor DRD5 expression. ONC201 is well…
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Keywords:
adult;
glioblastoma;
onc201;
recurrent glioblastoma ... See more keywords
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Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-1067
Abstract: Pancreatic cancer is a highly chemo-resistant tumor type known to aggressively metastasize at an early stage with an overall five-year survival rate of ~6%. In this study we tested the efficacy of ONC201 and ONC212…
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Keywords:
combination;
onc201;
cell lines;
pancreatic cancer ... See more keywords
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Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-3245
Abstract: We previously identified a novel, potent anti-cancer small molecule ONC201, which upregulates the integrated stress response (ISR) through ATF4/CHOP/DR5 and acts as a dual inactivator of Akt and ERK, leading to TRAIL gene activation. After…
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Keywords:
imipridone;
onc201;
potent anti;
family ... See more keywords
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Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-4914
Abstract: ONC201 is the first bitopic dopamine receptor D2 (DRD2) antagonist and allosteric mitochondrial protease ClpP agonist. Downstream of target engagement, ONC201 activates the integrated stress response pathway resulting in selective tumor cell death. ONC201 is…
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Keywords:
onc201 onc206;
onc201;
clpp;
cell lines ... See more keywords
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Published in 2019 at "Journal for Immunotherapy of Cancer"
DOI: 10.1186/s40425-019-0599-8
Abstract: BackgroundONC201 is a small molecule antagonist of DRD2, a G protein-coupled receptor overexpressed in several malignancies, that has prolonged antitumor efficacy and immunomodulatory properties in preclinical models. The first-in-human trial of ONC201 previously established a…
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Keywords:
advanced solid;
onc201;
enhanced immunostimulatory;
solid tumor ... See more keywords
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Published in 2017 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2017.35.15_suppl.2586
Abstract: 2586Background: ONC201 is an orally active, small molecule selective antagonist of the G protein-coupled receptor DRD2 that has established a new class of compounds referred to as imipridones. A first-in-human trial of ONC201 defined its…
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Keywords:
onc201;
anticancer immunostimulatory;
immunostimulatory activity;
drd2 ... See more keywords