ArticleProceedings of the National Academy of Sciences of the United States of America2008
Intermolecular interactions identify ligand-selective activity of estrogen receptor alpha/beta dimers.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
59 citing papers in PubMed, 1 synthesis or guideline pooled it, 105 citations in OpenAlex.
- The Role of Estrogen in Mitochondrial Disease.Cellular and molecular neurobiology · 2025Pooled it
- Molecular basis of azole fungicide interactions with human estrogen receptor alpha (ERα): an integrated in silico and in vitro toxicological assessment.Archives of toxicology · 2026Article
- Estrogen Receptor Beta Isoforms Interplay Integrates Nuclear and Extra-Nuclear Signaling to Modulate Human Granulosa Cell Growth.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2026Article
- Article
- Review
- Evolution of androgen receptors contributes to species variation in androgenic regulation of communication signals in electric fishes.Molecular and cellular endocrinology · 2023Article
- Article
- Article
- HMGB1 promotes the development of castration‑resistant prostate cancer by regulating androgen receptor activation.Oncology reports · 2022Article
- Polyamine Oxidase Expression Is Downregulated by 17β-Estradiol via Estrogen Receptor 2 in Human MCF-7 Breast Cancer Cells.International journal of molecular sciences · 2022Article
- Ginsenoside Rh2 inhibits breast cancer cell growth via ERβ-TNFα pathway.Acta biochimica et biophysica Sinica · 2022Article
- Repurposing the estrogen receptor modulator raloxifene to treat SARS-CoV-2 infection.Cell death and differentiation · 2022Review
- Estrogenic Pastures: A Source of Endocrine Disruption in Sheep Reproduction.Frontiers in endocrinology · 2022Review
- Development of a Human Estrogen Receptor Dimerization Assay for the Estrogenic Endocrine-Disrupting Chemicals Using Bioluminescence Resonance Energy Transfer.International journal of environmental research and public health · 2021Article
- The Calcium-Activated Chloride Channel TMEM16A is Inhibitied by Liquiritigenin.Frontiers in pharmacology · 2021Article
- Computer-Aided Ligand Discovery for Estrogen Receptor Alpha.International journal of molecular sciences · 2020Review
- Estrogen Receptors and Ubiquitin Proteasome System: Mutual Regulation.Biomolecules · 2020Review
- Nuclear estrogen receptor activation by insulin-like growth factor-1 in Neuro-2A neuroblastoma cells requires endogenous estrogen synthesis and is mediated by mutually repressive MAPK and PI3K cascades.Molecular and cellular endocrinology · 2019Article
- Sex-specific regulation of collagen I and III expression by 17β-Estradiol in cardiac fibroblasts: role of estrogen receptors.Cardiovascular research · 2019Article
- Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Estrogen receptor (ER) dimerization is prerequisite for its activation of target gene transcription. Because the two forms of ER, ERalpha and ERbeta, exhibit opposing functions in cell proliferation, the ability of ligands to induce ERalpha/beta heterodimers vs. their respective homodimers is expected to have profound impacts on transcriptional outcomes and cellular growth. However, there is a lack of direct methods to monitor the formation of ERalpha/beta heterodimers in vivo and to distinguish the ability of estrogenic ligands to promote ER homo- vs. heterodimerization. Here, we describe bioluminescence resonance energy transfer (BRET) assays for monitoring the formation of ERalpha/beta heterodimers and their respective homodimers in live cells. We demonstrate that although both partners contribute to heterodimerization, ligand-bound ERalpha plays a dominant role. Furthermore, a bioactive component was found to induce ERbeta/beta homodimers, and ERalpha/beta heterodimers but had minimal activity on ERalpha/alpha homodimers, posing a model that compounds promoting ERalpha/beta heterodimer formation might have therapeutic value. Thus, ER homodimer and heterodimer BRET assays are applicable to drug screening for dimer-selective selective ER modulators. Furthermore, this strategy can be used to study other nuclear receptor dimers.
Indexed as
Identifiers
What OpenQuestion holds
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.