Search Results - "Allen, Joshua E"
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A Bayesian machine learning approach for drug target identification using diverse data types
Published in Nature communications (19-11-2019)“…Drug target identification is a crucial step in development, yet is also among the most complex. To address this, we develop BANDIT, a Bayesian…”
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Small-Molecule ONC201/TIC10 Targets Chemotherapy-Resistant Colorectal Cancer Stem-like Cells in an Akt/Foxo3a/TRAIL-Dependent Manner
Published in Cancer research (Chicago, Ill.) (01-04-2015)“…Self-renewing colorectal cancer stem/progenitor cells (CSC) contribute to tumor maintenance and resistance to therapy. Therapeutic targeting of CSCs could…”
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ONC201 and imipridones: Anti-cancer compounds with clinical efficacy
Published in Neoplasia (New York, N.Y.) (01-12-2020)“…ONC201 was originally discovered as TNF-Related Apoptosis Inducing Ligand (TRAIL)-inducing compound TIC10. ONC201 appears to act as a selective antagonist of…”
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A phase 2 study of the first imipridone ONC201, a selective DRD2 antagonist for oncology, administered every three weeks in recurrent glioblastoma
Published in Oncotarget (03-10-2017)“…ONC201 is an oral, small molecule selective antagonist of the G protein-coupled receptor DRD2 that causes p53-independent apoptosis in tumor cells via…”
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Leveraging external data in the design and analysis of clinical trials in neuro-oncology
Published in The lancet oncology (01-10-2021)“…Integration of external control data, with patient-level information, in clinical trials has the potential to accelerate the development of new treatments in…”
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Role of Dopamine Receptors in the Anticancer Activity of ONC201
Published in Neoplasia (New York, N.Y.) (01-01-2018)“…ONC201/TIC10 is a first-in-class small molecule inducer of TRAIL that causes early activation of the integrated stress response. Its promising safety profile…”
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Dual inactivation of Akt and ERK by TIC10 signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects
Published in Science translational medicine (06-02-2013)“…Recombinant tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is an antitumor protein that is in clinical trials as a potential anticancer…”
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ATF4 induction through an atypical integrated stress response to ONC201 triggers p53-independent apoptosis in hematological malignancies
Published in Science signaling (16-02-2016)“…The clinical challenge posed by p53 abnormalities in hematological malignancies requires therapeutic strategies other than standard genotoxic chemotherapies…”
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Imipridone ONC212 activates orphan G protein-coupled receptor GPR132 and integrated stress response in acute myeloid leukemia
Published in Leukemia (01-12-2019)“…Imipridones constitute a novel class of antitumor agents. Here, we report that a second-generation imipridone, ONC212, possesses highly increased antitumor…”
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First-In-Class Small Molecule ONC201 Induces DR5 and Cell Death in Tumor but Not Normal Cells to Provide a Wide Therapeutic Index as an Anti-Cancer Agent
Published in PloS one (18-11-2015)“…We previously identified ONC201 (TIC10) as a first-in-class orally active small molecule with robust antitumor activity that is currently in clinical trials in…”
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Regulation of the human TRAIL gene
Published in Cancer biology & therapy (01-10-2012)“…TRAIL is a member of the TNF superfamily that induces tumor-selective cell death by engaging the pro-apoptotic death receptors DR4 and DR5. The antitumor…”
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A novel dopamine receptor D2 antagonist (ONC206) potentiates the effects of olaparib in endometrial cancer
Published in Cancer biology & therapy (31-12-2023)“…Poly ADP-ribose polymerase (PARP) inhibitors are effective therapies for cancer patients with homologous recombination (HR) deficient tumors. The imipridone…”
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Preclinical evaluation of the imipridone family, analogs of clinical stage anti-cancer small molecule ONC201, reveals potent anti-cancer effects of ONC212
Published in Cell cycle (Georgetown, Tex.) (02-10-2017)“…Anti-cancer small molecule ONC201 upregulates the integrated stress response (ISR) and acts as a dual inactivator of Akt/ERK, leading to TRAIL gene activation…”
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Discovery and clinical introduction of first-in-class imipridone ONC201
Published in Oncotarget (08-11-2016)“…ONC201 is the founding member of a novel class of anti-cancer compounds called imipridones that is currently in Phase II clinical trials in multiple advanced…”
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Targeting dopamine receptor D2 as a novel therapeutic strategy in endometrial cancer
Published in Journal of experimental & clinical cancer research (08-02-2021)“…ONC201 is a dopamine receptor D2 (DRD2) antagonist that inhibits tumor growth in preclinical models through ClpP activation to induce integrated stress…”
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Modulating the unfolded protein response with ONC201 to impact on radiation response in prostate cancer cells
Published in Scientific reports (19-02-2021)“…Prostate cancer (PCa) is the most common non-cutaneous cancer in men and a notable cause of cancer mortality when it metastasises. The unfolded protein…”
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Cancer stem cell-related gene expression as a potential biomarker of response for first-in-class imipridone ONC201 in solid tumors
Published in PloS one (02-08-2017)“…Cancer stem cells (CSCs) correlate with recurrence, metastasis and poor survival in clinical studies. Encouraging results from clinical trials of CSC…”
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Genetic and Pharmacological Screens Converge in Identifying FLIP, BCL2, and IAP Proteins as Key Regulators of Sensitivity to the TRAIL-Inducing Anticancer Agent ONC201/TIC10
Published in Cancer research (Chicago, Ill.) (15-04-2015)“…ONC201/TIC10 is a small-molecule inducer of the TRAIL gene under current investigation as a novel anticancer agent. In this study, we identify critical…”
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ONC206, an Imipridone Derivative, Induces Cell Death Through Activation of the Integrated Stress Response in Serous Endometrial Cancer In Vitro
Published in Frontiers in oncology (20-10-2020)“…ONC206 (Oncoceutics) is an imipiridone with nanomolar potency and analogue of ONC201, a selective dopamine receptor D2 (DRD2) antagonist currently being…”
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Anti-Tumor and Anti-Invasive Effects of ONC201 on Ovarian Cancer Cells and a Transgenic Mouse Model of Serous Ovarian Cancer
Published in Frontiers in oncology (17-03-2022)“…ONC201 is a promising first-in-class small molecule that has been reported to have anti-neoplastic activity in various types of cancer through activation of…”
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