ArticleInternational journal of molecular sciences2023
Phenylsulfonimide PPARα Antagonists Enhance Nrf2 Activation and Promote Oxidative Stress-Induced Apoptosis/Pyroptosis in MCF7 Breast Cancer Cells.
Article in International journal of molecular sciences, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 17 citations in OpenAlex.
- The role of NRF2 in human cancers: Pre-clinical insights paving the way for clinical trials.Journal of pharmaceutical analysis · 2026Review
- Insulin Resistance and Inflammation.International journal of molecular sciences · 2026Review
- Hybridization Approach Applied to Umbelliferon and Vanilloids toward New Inhibitors of Carbonic Anhydrases IX and XII with In Vitro Antiproliferative and Anti-inflammatory Activities.Journal of medicinal chemistry · 2026Article
- Organelles and cancer cell pyroptosis: overview and perspectives.Cell death & disease · 2025Review
- Ethanolic Extract ofPharmaceuticals (Basel, Switzerland) · 2025Article
- Article
- Investigation on Human Carbonic Anhydrase IX and XII Inhibitory Activity and A549 Antiproliferative Activity of a New Class of Coumarinamides.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Durvalumab and T-DXd Synergistically Promote Apoptosis of Cholangiocarcinoma Cells by Downregulating EGR1 Expression Through Inhibiting P38 MAPK Pathway.Applied biochemistry and biotechnology · 2025Article
- Role of Peroxisome Proliferator-Activated Receptor α-Dependent Mitochondrial Metabolism in Ovarian Cancer Stem Cells.International journal of molecular sciences · 2024Article
- ROS induced pyroptosis in inflammatory disease and cancer.Frontiers in immunology · 2024Review
- Effect of tumor-associated macrophages on the pyroptosis of breast cancer tumor cells.Cell communication and signaling : CCS · 2023Review
- Pyroptosis Modulators: New Insights of Gasdermins in Health and Disease.Antioxidants (Basel, Switzerland) · 2023Review
- Modeling of senescence-related chemoresistance in ovarian cancer using data analysis and patient-derived organoids.Frontiers in oncology · 2023Article
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Authors and funding
7 authors at 1 institution in 1 country.
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Abstract
The NF-E2-related factor 2 transcription factor (Nrf2) orchestrates the basal and stress-inducible activation of a vast array of antioxidant genes. A high amount of reactive oxygen species (ROS) promotes carcinogenesis in cells with defective redox-sensitive signaling factors such as Nrf2. In breast cancer (BC), emerging evidence indicates that increased Nrf2 activity enhances cell metastatic potential. An interconnection between peroxisome proliferator-activated receptors (PPARs) and Nrf2 pathways in cancer has been shown. In this light, newly synthesized PPARα antagonists, namely IB42, IB44, and IB66, were tested in the BC cell line MCF7 in parallel with GW6471 as the reference compound. Our results show that the most promising compound of this phenylsulfonimide series (IB66) is able to decrease MCF7 proliferation by blocking cells at the G2/M checkpoint. The underlying mechanism has been investigated, disclosing a caspase 3/Akt-dependent apoptotic/pyroptotic pathway induced by the increased generation of oxidative stress. Moreover, the involvement of Nrf2 and COX2 in IB66-treated MCF7 cell response has been highlighted. The reported data lay the groundwork for the development of alternative targeted therapy involving the Nrf2/PPARα molecular axis, able to overcome BC cell chemoresistance and cause better clinical outcomes, promoting other forms of programmed cell death, such as pyroptosis.
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