BET inhibition disrupts the FOXM1-MYC axis to induce BRCAness and enhance PARP inhibitor response

Homologous recombination (HR) proficiency underlies intrinsic and acquired resistance to PARP inhibitors (PARPi). We identify a BRD4-dependent FOXM1-MYC transcriptional axis that sustains HR gene expression and limits PARPi response. ENCODE analyses revealed extensive co-occupancy of FOXM1 and MYC at regulatory regions of DNA repair genes, including BRCA1/2 and RAD51 paralogs, suggesting a shared HR program. Functionally, transient knockdown of FOXM1 or MYC reduced BRCA1/RAD51 transcripts, whereas sustained FOXM1 silencing triggered adaptive MYC upregulation that preserved HR output, indicating compensatory control. BET inhibition with (+)-JQ1 diminished FOXM1/MYC promoter occupancy at BRCA1 and RAD51, downregulated HR genes, and synergized with PARPi in viability and clonogenic assays. A BRD4 degrader (ZBC260) achieved potent BRD4 depletion at low nanomolar doses, suppressed FOXM1/MYC and HR gene expression, enhanced PARP1 trapping, and produced strong synergy with olaparib, including in patient-derived cancer cells. Clinically, BRD4 is highly expressed in ovarian cancer and independently predicts poor survival, outperforming FOXM1 and MYC. These data establish BRD4-directed disruption of the FOXM1-MYC axis as a strategy to induce "BRCAness" and broaden PARPi efficacy.

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Journal
npj Precision Oncology
Published
2026-03-12
DOI
https://doi.org/10.1038/s41698-026-01360-x
Primary Topic
Protein Degradation and Inhibitors
Type
article
Field-Weighted Citation Impact
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article

BET inhibition disrupts the FOXM1-MYC axis to induce BRCAness and enhance PARP inhibitor response

Jeremy Chien, Rebecca Brooks, Gary S. Leiserowitz, Kay Minn et al.
npj Precision Oncology
Protein Degradation and Inhibitors
article

BET inhibition disrupts the FOXM1-MYC axis to induce BRCAness and enhance PARP inhibitor response

Jeremy Chien, Rebecca Brooks, Gary S. Leiserowitz, Kay Minn, Anais Saunders, Katherine Jane Chua, Danika Bakke, Pingping Fang, Shaomeng Wang, Neil Johnson
article en

Abstract

Homologous recombination (HR) proficiency underlies intrinsic and acquired resistance to PARP inhibitors (PARPi). We identify a BRD4-dependent FOXM1-MYC transcriptional axis that sustains HR gene expression and limits PARPi response. ENCODE analyses revealed extensive co-occupancy of FOXM1 and MYC at regulatory regions of DNA repair genes, including BRCA1/2 and RAD51 paralogs, suggesting a shared HR program. Functionally, transient knockdown of FOXM1 or MYC reduced BRCA1/RAD51 transcripts, whereas sustained FOXM1 silencing triggered adaptive MYC upregulation that preserved HR output, indicating compensatory control. BET inhibition with (+)-JQ1 diminished FOXM1/MYC promoter occupancy at BRCA1 and RAD51, downregulated HR genes, and synergized with PARPi in viability and clonogenic assays. A BRD4 degrader (ZBC260) achieved potent BRD4 depletion at low nanomolar doses, suppressed FOXM1/MYC and HR gene expression, enhanced PARP1 trapping, and produced strong synergy with olaparib, including in patient-derived cancer cells. Clinically, BRD4 is highly expressed in ovarian cancer and independently predicts poor survival, outperforming FOXM1 and MYC. These data establish BRD4-directed disruption of the FOXM1-MYC axis as a strategy to induce "BRCAness" and broaden PARPi efficacy.

npj Precision Oncology
Fox Chase Cancer Center (US), University of Michigan (US), University of California System (US), Novogene Bioinformatics Institute (CN), University of Kansas Medical Center (US), Caris Life Sciences (United States) (US), University of California, Davis (US)
Openalex Percentile: Top 26%
Protein Degradation and Inhibitors
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