Evidence mapPaperPMID 37069726Full record

ArticleCancer biology & therapy2023

A novel dopamine receptor D2 antagonist (ONC206) potentiates the effects of olaparib in endometrial cancer.

Sarah E Paraghamian, Jianqing Qiu, Gabrielle M Hawkins, Ziyi Zhao, Wenchuan Sun, Yali Fan, Xin Zhang, Hongyan Suo, Tianran Hao, Varun Vijay Prabhu and 3 more

Open access · goldAbstract read
In one paragraph

Article in Cancer biology & therapy, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
2.1field-weighted citation impact, top 12% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

8 citing papers in PubMed, 9 citations in OpenAlex.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

13 authors at 3 institutions in 2 countries.

Sarah E ParaghamianDivision of Gynecologic Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
Jianqing QiuDepartment of Obstetrics and Gynecology, the Second Hospital of Shandong University, Jinan, China.
Gabrielle M HawkinsDivision of Gynecologic Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
Ziyi ZhaoDivision of Gynecologic Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
Wenchuan SunDivision of Gynecologic Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
Yali FanDivision of Gynecologic Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
Xin ZhangDivision of Gynecologic Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
Hongyan SuoDivision of Gynecologic Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
Tianran HaoDivision of Gynecologic Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
Varun Vijay PrabhuChimerix, Durham, NC, USA.
Joshua E AllenChimerix, Durham, NC, USA.
Chunxiao ZhouDivision of Gynecologic Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.ORCID 0000-0002-1257-9537
Victoria Bae-JumpDivision of Gynecologic Oncology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
University of North Carolina at Chapel Hill · USChimerix (United States) · USSecond Hospital of Shandong University · CN

Funding

Obesity-driven Metabolic and Molecular Biomarkers of Metformin Response in Endometrial CancerR37CA226969 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI BAE-JUMP, VICTORIA LIN · 2018 to 2024
$2.5M
NCI NIH HHS R37 CA226969
6 · The paper itself

Abstract

Poly ADP-ribose polymerase (PARP) inhibitors are effective therapies for cancer patients with homologous recombination (HR) deficient tumors. The imipridone ONC206 is an orally bioavailable dopamine receptor D2 antagonist and mitochondrial protease ClpP agonist that has anti-tumorigenic effects in endometrial cancer via induction of apoptosis, activation of the integrated stress response and modulation of PI3K/AKT signaling. Both PARP inhibitors and imipridones are being evaluated in endometrial cancer clinical trials but have yet to be explored in combination. In this manuscript, we evaluated the effects of the PARP inhibitor olaparib in combination with ONC206 in human endometrioid endometrial cancer cell lines and in a genetically engineered mouse model of endometrial cancer. Our results showed that simultaneous exposure of endometrial cancer cells to olaparib and ONC206 resulted in synergistic anti-proliferative effects and increased cellular stress and apoptosis in both cell lines, compared to either drug alone. The combination treatment also decreased expression of the anti-apoptotic protein Bcl-2 and reduced phosphorylation of AKT and S6, with greater effects compared to either drug alone. In the transgenic model of endometrial cancer, the combination of olaparib and ONC206 resulted in a more significant reduction in tumor weight in obese and lean mice compared to ONC206 alone or olaparib alone, together with a considerably decreased Ki-67 and enhanced H2AX expression in obese and lean mice. These results suggest that this novel dual therapy may be worthy of further exploration in clinical trials.

Indexed as

Antineoplastic AgentsEndometrial NeoplasmsAnimalsCell Line, TumorCell ProliferationFemaleHumansMicePhosphatidylinositol 3-KinasesPhthalazinesPiperazinesPoly(ADP-ribose) Polymerase InhibitorsProto-Oncogene Proteins c-aktReceptors, DopamineAntineoplastic AgentsolaparibPhosphatidylinositol 3-KinasesPhthalazinesPiperazinesPoly(ADP-ribose) Polymerase InhibitorsProto-Oncogene Proteins c-aktReceptors, Dopamineapoptosisendometrial cancerolaparibONC206synergy

Identifiers

PMID37069726
PMCPMC10115124
OpenAlexW4366242359

What Socratic holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.