ArticleMolecular endocrinology (Baltimore, Md.)2010
Regulation of aryl hydrocarbon receptor function by selective estrogen receptor modulators.
Article in Molecular endocrinology (Baltimore, Md.), 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
28 citing papers in PubMed, 55 citations in OpenAlex.
- Review
- Aryl hydrocarbon receptor (AhR)-mediated signaling as a critical regulator of skeletal cell biology.Journal of molecular endocrinology · 2022Review
- The inhibition of tamoxifen on UGT2B gene expression and enzyme activity in rat liver contribute to the estrogen homeostasis dysregulation.BMC pharmacology & toxicology · 2022Article
- The Ahr2-Dependent wfikkn1 Gene Influences Zebrafish Transcriptome, Proteome, and Behavior.Toxicological sciences : an official journal of the Society of Toxicology · 2022Article
- The Prognostic Impact of Intratumoral Aryl Hydrocarbon Receptor in Primary Breast Cancer Depends on the Type of Endocrine Therapy: A Population-Based Cohort Study.Frontiers in oncology · 2021Article
- Developmental malformations resulting from high-dose maternal tamoxifen exposure in the mouse.PloS one · 2021Article
- Impact of AHR Ligand TCDD on Human Embryonic Stem Cells and Early Differentiation.International journal of molecular sciences · 2020Article
- Review
- The Aryl Hydrocarbon Receptor: Connecting Immunity to the Microenvironment.Trends in immunology · 2018Review
- AhR ligand aminoflavone suppresses α6-integrin-Src-Akt signaling to attenuate tamoxifen resistance in breast cancer cells.Journal of cellular physiology · 2018Article
- The Aryl Hydrocarbon Receptor (AhR) as a Drug Target for Cancer Chemotherapy.Current opinion in toxicology · 2017Article
- Estrogen receptor-α and aryl hydrocarbon receptor involvement in the actions of botanical estrogens in target cells.Molecular and cellular endocrinology · 2016Article
- Collagen density regulates xenobiotic and hypoxic response of mammary epithelial cells.Environmental toxicology and pharmacology · 2015Article
- The aryl hydrocarbon receptor ligand omeprazole inhibits breast cancer cell invasion and metastasis.BMC cancer · 2014Article
- Aryl hydrocarbon receptor deficiency causes dysregulated cellular matrix metabolism and age-related macular degeneration-like pathology.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- Role of the aryl hydrocarbon receptor in carcinogenesis and potential as a drug target.Toxicological sciences : an official journal of the Society of Toxicology · 2013Review
- Aryl hydrocarbon receptor (AHR)-active pharmaceuticals are selective AHR modulators in MDA-MB-468 and BT474 breast cancer cells.The Journal of pharmacology and experimental therapeutics · 2012Article
- Alkylphenols--potential modulators of the allergic response.The Kaohsiung journal of medical sciences · 2012Review
- The aryl hydrocarbon receptor mediates leflunomide-induced growth inhibition of melanoma cells.PloS one · 2012Article
- Transcriptional signatures of regulatory and toxic responses to benzo-[a]-pyrene exposure.BMC genomics · 2011Article
Corrections and comments
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Authors and funding
8 authors at 5 institutions in 1 country.
Funding
Abstract
Selective estrogen receptor modulators (SERMs), such as tamoxifen (TAM), have been used extensively for the treatment and prevention of breast cancer and other pathologies associated with aberrant estrogen receptor (ER) signaling. These compounds exhibit cell-selective agonist/antagonist activities as a consequence of their ability to induce different conformational changes in ER, thereby enabling it to recruit functionally distinct transcriptional coregulators. However, the observation that SERMs can also regulate aspects of calcium signaling and apoptosis in an ER-independent manner in some systems suggests that some of the activity of drugs within this class may also arise as a consequence of their ability to interact with targets other than ER. In this study, we demonstrate that 4-hydroxy-TAM (4OHT), an active metabolite of TAM, directly binds to and modulates the transcriptional activity of the aryl hydrocarbon receptor (AHR). Of specific interest was the observation, that in the absence of ER, 4OHT can induce the expression of AHR target genes involved in estradiol metabolism, cellular proliferation, and metastasis in cellular models of breast cancer. The potential role for AHR in SERM pharmacology was further underscored by the ability of 4OHT to suppress osteoclast differentiation in vitro in part through AHR. Cumulatively, these findings provide evidence that it is necessary to reevaluate the relative roles of ER and AHR in manifesting the pharmacological actions and therapeutic efficacy of TAM and other SERMs.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.