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Pancreatic ductal adenocarcinoma (PDAC) remains one of the deadliest cancers demanding better and more effective therapies. BARD1 or BRCA1-Associated -Ring Domain-1 plays a pivotal role in homologous recombination repair (HRR). However, its function and the underlying molecular mechanisms in PDAC are still not fully elucidated. Here, we demonstrate that BARD1 is overexpressed in PDAC and its genetic inhibition suppresses c-Myc and disrupts c-Myc dependent transcriptional program. Mechanistically, BARD1 stabilizes c-Myc through ubiquitin-proteasome system by regulating FBXW7. Importantly, targeting BARD1 using either siRNAs or CRISPR/Cas9 deletion blocks PDAC growth in vitro and in vivo, without any signs of toxicity to mice. Using a focused drug library of 477 DNA damage response compounds, we also found that BARD1 inhibition enhances therapeutic efficacy of several clinically relevant agents (fold changes ≥4), including PARPi, in HRR proficient PDAC cells. These data uncover BARD1 as an attractive therapeutic target for HRR proficient PDAC.
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http://dx.doi.org/10.1016/j.neo.2025.101152 | DOI Listing |
Cell Rep Med
August 2025
Department of Gynecologic Oncology and Reproductive Medicine, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA. Electronic address:
Despite the clinical use of anti-vascular endothelial growth factor (VEGF) antibodies (AVAs) in cancer therapy, resistance frequently develops, leading to disease progression. To address this, we identify a previously unknown role for breast cancer type 1 susceptibility protein (BRCA1)-associated RING domain 1 (BARD1) in modulating AVA sensitivity. Epigenetic modulation-via global and targeted DNA methylation-reveals BARD1 as a key regulator of angiogenesis.
View Article and Find Full Text PDFDiscov Oncol
August 2025
Department of Biotechnology, Indian Institute of Technology Hyderabad, Kandi, Sangareddy, 502285, India.
Introduction: Castration-resistant prostate cancer (CRPC) poses a major clinical challenge due to its aggressive nature, therapeutic resistance, and frequent progression to bone metastasis. Emerging evidence suggests that E3 ubiquitin ligases play a key role in cancer progression, yet their involvement in CRPC remains poorly understood.
Methods And Results: In this study, we employed machine learning (ML) algorithms and integrative bioinformatics approaches to analyze the gene expression profiles of E3 ubiquitin ligases in CRPC patients.
J Phys Chem B
August 2025
Departments of Biochemistry & Biophysics and Bioengineering, University of Pennsylvania, Philadelphia, Pennsylvania 19104, United States.
Mechanistic insight into biophysical perturbations caused by pathogenic missense mutations is highly valuable information for the rational design of therapeutics. For hereditary breast and ovarian cancers, multiple pathogenic mutations in the N-terminal domain of have been reported in patients. How exactly these mutations disrupt the catalytic activity of , and thereby lead to oncogenesis, is unknown.
View Article and Find Full Text PDFGastric Cancer
July 2025
Department of Oncology, Asan Medical Center, University of Ulsan College of Medicine, 88, Olympic-ro 43-gil, Songpa-gu, Seoul, 05505, Republic of Korea.
Background: Homologous recombination repair (HRR) gene mutations contribute to genomic instability. However, their clinical value in immune checkpoint inhibitor (ICI)-based treatments in gastric cancer remains unclear. Therefore, this study aims to investigate the efficacy of nivolumab plus chemotherapy according to the HRR mutation status in patients with advanced gastric cancer.
View Article and Find Full Text PDFbioRxiv
June 2025
Departments of Biochemistry & Biophysics and Bioengineering, University of Pennsylvania, Philadelphia, PA 19104, United States.
Mechanistic insight into biophysical perturbations caused by pathogenic missense mutations is highly valuable information for the rational design of therapeutics. For hereditary breast and ovarian cancer, multiple pathogenic mutations in the N-terminal domain of have been reported in patients. How exactly these mutations disrupt the catalytic activity of , and thereby lead to oncogenesis, is unknown.
View Article and Find Full Text PDF