ArticleMolecular cancer research : MCR2012
Ah receptor antagonism represses head and neck tumor cell aggressive phenotype.
Article in Molecular cancer research : MCR, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 50 papers.
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Who cites it
50 citing papers in PubMed, 73 citations in OpenAlex.
- IK-175, an Oral Aryl Hydrocarbon Receptor Inhibitor, Alone and with Nivolumab in Patients with Advanced Solid Tumors and Urothelial Carcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research · 2026Article
- Circadian rhythm and aryl hydrocarbon receptor crosstalk in bone marrow adipose tissue and implications in leukemia.Scientific reports · 2025Article
- Combination screen in multi-cell type tumor spheroids reveals interaction between aryl hydrocarbon receptor antagonists and E1 ubiquitin-activating enzyme inhibitor.SLAS discovery : advancing life sciences R & D · 2024Article
- High indoleamine 2,3-dioxygenase transcript levels predict better outcome after front-line cancer immunotherapy.iScience · 2024Article
- Human Papilloma Virus Positive Oropharyngeal Squamous Cell Carcinoma and the Immune System: Pathogenesis, Immunotherapy and Future Perspectives.International journal of molecular sciences · 2024Review
- The aryl hydrocarbon receptor as a tumor modulator: mechanisms to therapy.Frontiers in oncology · 2024Review
- Long-term exposure to BAY2416964 reduces proliferation, migration and recapitulates transcriptional changes induced by AHR loss in PyMT-induced mammary tumor cells.Frontiers in oncology · 2024Article
- Exploring aryl hydrocarbon receptor expression and distribution in the tumor microenvironment, with a focus on immune cells, in various solid cancer types.Frontiers in immunology · 2024Article
- Patterns of Carbon-Bound Exogenous Compounds Impact Disease Pathophysiology in Lung Cancer Subtypes in Different Ways.ACS nano · 2023Article
- Tumor-Suppressive Functions of the Aryl Hydrocarbon Receptor (AhR) and AhR as a Therapeutic Target in Cancer.Biology · 2023Review
- Health Benefits of Coffee Consumption for Cancer and Other Diseases and Mechanisms of Action.International journal of molecular sciences · 2023Review
- Indoleamine 2,3-dioxygenase (IDO) inhibitors and cancer immunotherapy.Cancer treatment reviews · 2022Review
- VEGF-B targeting by aryl hydrocarbon receptor mediates the migration and invasion of choriocarcinoma stem-like cells.Cancer cell international · 2022Article
- Stemness and immune evasion conferred by the TDO2-AHR pathway are associated with liver metastasis of colon cancer.Cancer science · 2022Article
- Multidrug efflux transporter ABCG2: expression and regulation.Cellular and molecular life sciences : CMLS · 2021Review
- IL-6 in the Ecosystem of Head and Neck Cancer: Possible Therapeutic Perspectives.International journal of molecular sciences · 2021Review
- The aryl hydrocarbon receptor suppresses immunity to oral squamous cell carcinoma through immune checkpoint regulation.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Chemokine-Cytokine Networks in the Head and Neck Tumor Microenvironment.International journal of molecular sciences · 2021Review
- Association Between Interleukin-6 and Head and Neck Squamous Cell Carcinoma: A Systematic Review.Clinical and experimental otorhinolaryngology · 2021Review
- AhR and Cancer: From Gene Profiling to Targeted Therapy.International journal of molecular sciences · 2021Review
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
Abstract
The aryl hydrocarbon receptor (AhR) has been shown to play a role in an increasing number of cellular processes. Recent reports have linked the AhR to cell proliferation, cytoskeletal arrangement, and tumor invasiveness in various tumor cell types. The AhR plays a role in the de-repression of the interleukin (IL)6 promoter in certain tumor cell lines, allowing for increased transcriptional activation by cytokines. Here, we show that there is a significant level of constitutive activation of the AhR in cells isolated from patients with head and neck squamous cell carcinoma (HNSCC). Constitutive activation of the AhR in HNSCCs was blocked by antagonist treatment, leading to a reduction in IL6 expression. In addition, the AhR exhibits a high level of expression in HNSCCs than in normal keratinocytes. These findings led to the hypothesis that the basal AhR activity in HNSCCs plays a role in the aggressive phenotype of these tumors and that antagonist treatment could mitigate this phenotype. This study provides evidence that antagonism of the AhR in HNSCC tumor cells, in the absence of exogenous receptor ligands, has a significant effect on tumor cell phenotype. Treatment of these cell lines with the AhR antagonists 6, 2', 4'-trimethoxyflavone, or the more potent GNF351, decreased migration and invasion of HNSCC cells and prevented benzo[a]pyrene-mediated induction of the chemotherapy efflux protein ABCG2. Thus, an AhR antagonist treatment has been shown to have therapeutic potential in HNSCCs through a reduction in aggressive cell phenotype.
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