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Abstract B142: EO3001: A novel agent for ARID1A mutant cancers

2025· article· en· W4415444393 on OpenAlexaff
Jeffrey Bacha, Yuchen Ding, Dennis Brown, Amal M. El-Naggar, David G. Huntsman, Sarath Kanekal, Neil Sankar

Bibliographic record

VenueMolecular Cancer Therapeutics · 2025
Typearticle
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicChromatin Remodeling and Cancer
Canadian institutionsBC Cancer Agency
Fundersnot available
KeywordsARID1AOxidative stressCancerCell cultureEx vivoChromatin remodelingMitochondrionIn vivoCellCell growth

Abstract

fetched live from OpenAlex

Abstract Background ARID1A mutations are among the most common genetic alterations in cancer, occurring in approximately 65% of ovarian clear cell carcinoma (OCCC) and up to 10% of all solid tumors. These mutations disrupt chromatin remodeling and cellular homeostasis, leading to the accumulation of reactive oxygen species (ROS) and a metabolic shift that renders tumor cells increasingly dependent on oxidative phosphorylation (OXPHOS) for survival. This metabolic vulnerability provides a therapeutic opportunity for selective targeting. EO3001 is a novel synthetic agent that transports extracellular Cu(II) to mitochondria, promoting mitochondrial ROS generation and triggering cancer cell death. Preclinical studies have shown that EO3001 exhibits selective cytotoxicity in ARID1A-deficient CCOC models, highlighting its potential as a precision oncology candidate. Methods To evaluate EO3001’s activity, isogenic CCOC cell lines with and without ARID1A expression were generated using CRISPR-Cas9 gene editing. The compound’s effects were assessed through a series of in vitro and ex vivo assays, measuring cell viability, mitochondrial ROS levels, OXPHOS activity, and invasive potential under various metabolic stress conditions. Notably, EO3001 demonstrated robust anti-tumor activity in ARID1A-deficient cells, with markedly reduced efficacy in hypoxic environments—supporting the mechanism of action linked to OXPHOS dependence. Conclusions and Next Steps These findings suggest that EO3001 holds promise as a targeted therapeutic for ARID1A-mutant cancers, and ongoing work is focused on optimizing its application in clinically relevant settings. A biomarker-driven clinical trial is planed to further evaluate these findings. Citation Format: Jeffrey Bacha, Yuchen Ding, Dennis Brown, Amal M. El-Naggar, David G. Huntsman, Sarath Kanekal, Neil Sankar. EO3001: A novel agent for ARID1A mutant cancers [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; 2025 Oct 22-26; Boston, MA. Philadelphia (PA): AACR; Mol Cancer Ther 2025;24(10 Suppl):Abstract nr B142.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.352
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.026
GPT teacher head0.315
Teacher spread0.289 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations0
Published2025
Admission routes1
Has abstractyes

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