ArticleEuropean journal of pharmacology2017
Phenylmethimazole and a thiazole derivative of phenylmethimazole inhibit IL-6 expression by triple negative breast cancer cells.
Article in European journal of pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 20 citations in OpenAlex.
- Integrated computational and preclinical evaluation of novel synthetic pyrazole pyrazoline thiazole derivative for breast cancer therapeutics.Scientific reports · 2025Article
- Docking and structure activity relationship studies of potent and selective thiazolidinethione GSK-3 inhibitors.Bioorganic & medicinal chemistry letters · 2025Article
- Small molecule agents for triple negative breast cancer: Current status and future prospects.Translational oncology · 2024Review
- Editorial: Toll-like receptor expression in transformed cells: role in tumor development and cancer therapies.Frontiers in immunology · 2024Article
- Toll‑like receptor 3 ligands for breast cancer therapies (Review).Molecular and clinical oncology · 2023Review
- Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Hormonal Regulation of the MHC Class I Gene in Thyroid Cells: Role of the Promoter "Tissue-Specific" Region.Frontiers in endocrinology · 2021Article
- Modulation of LPS-induced inflammatory cytokine production by a novel glycogen synthase kinase-3 inhibitor.European journal of pharmacology · 2020Article
- Celastrol Inhibits Migration and Invasion of Triple-Negative Breast Cancer Cells by Suppressing Interleukin-6 via Downregulating Nuclear Factor-κB (NF-κB).Medical science monitor : international medical journal of experimental and clinical research · 2020Article
- Identification of a novel selective and potent inhibitor of glycogen synthase kinase-3.American journal of physiology. Cell physiology · 2019Article
- TIMP3 Overexpression Improves the Sensitivity of Osteosarcoma to Cisplatin by Reducing IL-6 Production.Frontiers in genetics · 2018Article
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
Abstract
Inhibition of interleukin-6 (IL-6) holds significant promise as a therapeutic approach for triple negative breast cancer (TNBC). We previously reported that phenylmethimazole (C10) reduces IL-6 expression in several cancer cell lines. We have identified a more potent derivative of C10 termed COB-141. In the present work, we tested the hypothesis that C10 and COB-141 inhibit TNBC cell expressed IL-6 and investigated the potential for classical IL-6 pathway induced signaling within TNBC cells. A panel of TNBC cell lines (MDA-MB-231, Hs578T, MDA-MB-468) was used. Enzyme linked immunosorbent assays (ELISA) revealed that C10 and COB-141 inhibit MDA-MB-231 cell IL-6 secretion, with COB-141 being ~6.5 times more potent than C10. Therefore, the remainder of the study focused on COB-141 which inhibited IL-6 secretion, and was found, via quantitative real time polymerase chain reaction (QRT-PCR), to inhibit IL-6 mRNA in the TNBC panel. COB-141 had little, if any, effect on metabolic activity indicating that the IL-6 inhibition is not via a toxic effect. Flow cytometric analysis and QRT-PCR revealed that the TNBC cell lines do not express the IL-6 receptor (IL-6Rα). Trans-AM assays suggested that COB-141 exerts its inhibitory effect, at least in part, by reducing NF-κB (p65/p50) DNA binding. In summary, COB-141 is a potent inhibitor of TNBC cell expressed IL-6 and the inhibition does not appear to be due to non-specific toxicity. The TNBC cell lines do not have an intact classical IL-6 signaling pathway. COB-141's inhibitory effect may be due, at least in part, to reducing NF-κB (p65/p50) DNA binding.
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