ArticlePloS one2012
Identification of estrogen receptor dimer selective ligands reveals growth-inhibitory effects on cells that co-express ERα and ERβ.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
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Who cites it
41 citing papers in PubMed.
- Targeting Estrogen Receptor Beta in a Phase 2 Study of High-Dose Estradiol in Metastatic Triple-Negative Breast Cancer: A Wisconsin Oncology Network Study.Clinical breast cancer · 2016Trial
- 27-Hydroxycholesterol in bile duct tissue promotes cholangiocarcinoma progression through estrogen receptor signaling.American journal of cancer research · 2026Article
- Angolensin Isolated fromInternational journal of molecular sciences · 2025Article
- Novel Estrogen Receptor Dimerization BRET-Based Biosensors for Screening Estrogenic Endocrine-Disrupting Chemicals.Biomaterials research · 2024Article
- Significant Association of Estrogen Receptor-β Isoforms and Coactivators in Breast Cancer Subtypes.Current issues in molecular biology · 2023Article
- ERβ1 Sensitizes and ERβ2 Desensitizes ERα-Positive Breast Cancer Cells to the Inhibitory Effects of Tamoxifen, Fulvestrant and Their Combination with All-Trans Retinoic Acid.International journal of molecular sciences · 2023Article
- Cell Uptake of Steroid-BODIPY Conjugates and Their Internalization Mechanisms: Cancer Theranostic Dyes.International journal of molecular sciences · 2023Article
- ERβ Isoforms Have Differential Clinical Significance in Breast Cancer Subtypes and Subgroups.Current issues in molecular biology · 2022Article
- Estrogen Receptor β Expression and Its Clinical Implication in Breast Cancers: Favorable or Unfavorable?Journal of breast cancer · 2022Review
- Review
- Computer-Aided Ligand Discovery for Estrogen Receptor Alpha.International journal of molecular sciences · 2020Review
- Therapeutic potential of quercetin on human breast cancer in different dimensions.Inflammopharmacology · 2020Review
- Functional characterization of the ZEB2 regulatory landscape.Human molecular genetics · 2019Article
- PES1 promotes the occurrence and development of papillary thyroid cancer by upregulating the ERα/ERβ protein ratio.Scientific reports · 2019Article
- Unraveling the transcriptional regulation of TWIST1 in limb development.PLoS genetics · 2018Article
- Monitoring ligand-dependent assembly of receptor ternary complexes in live cells by BRETFect.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- A Computational-Based Approach to Identify Estrogen ReceptorMolecular pharmacology · 2018Article
- Protein biomarkers for subtyping breast cancer and implications for future research.Expert review of proteomics · 2018Review
- Cosmosiin Increases ADAM10 Expression via Mechanisms Involving 5'UTR and PI3K Signaling.Frontiers in molecular neuroscience · 2018Article
- Flexible small molecular anti-estrogens with N,N-dialkylated-2,5-diethoxy-4-morpholinoaniline scaffold targets multiple estrogen receptor conformations.Cell cycle (Georgetown, Tex.) · 2017Article
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
Estrogens play essential roles in the progression of mammary and prostatic diseases. The transcriptional effects of estrogens are transduced by two estrogen receptors, ERα and ERβ, which elicit opposing roles in regulating proliferation: ERα is proliferative while ERβ is anti-proliferative. Exogenous expression of ERβ in ERα-positive cancer cell lines inhibits cell proliferation in response to estrogen and reduces xenografted tumor growth in vivo, suggesting that ERβ might oppose ERα's proliferative effects via formation of ERα/β heterodimers. Despite biochemical and cellular evidence of ERα/β heterodimer formation in cells co-expressing both receptors, the biological roles of the ERα/β heterodimer remain to be elucidated. Here we report the identification of two phytoestrogens that selectively activate ERα/β heterodimers at specific concentrations using a cell-based, two-step high throughput small molecule screen for ER transcriptional activity and ER dimer selectivity. Using ERα/β heterodimer-selective ligands at defined concentrations, we demonstrate that ERα/β heterodimers are growth inhibitory in breast and prostate cells which co-express the two ER isoforms. Furthermore, using Automated Quantitative Analysis (AQUA) to examine nuclear expression of ERα and ERβ in human breast tissue microarrays, we demonstrate that ERα and ERβ are co-expressed in the same cells in breast tumors. The co-expression of ERα and ERβ in the same cells supports the possibility of ERα/β heterodimer formation at physio- and pathological conditions, further suggesting that targeting ERα/β heterodimers might be a novel therapeutic approach to the treatment of cancers which co-express ERα and ERβ.
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