ArticleThe Journal of biological chemistry2011
Exploration of dimensions of estrogen potency: parsing ligand binding and coactivator binding affinities.
Article in The Journal of biological chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers, 1 of them a synthesis that pooled it.
What it found
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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
34 citing papers in PubMed, 1 synthesis or guideline pooled it, 94 citations in OpenAlex.
- Higher Circulating Cortisol in the Follicular vs. Luteal Phase of the Menstrual Cycle: A Meta-Analysis.Frontiers in endocrinology · 2020Pooled it
- Effect of oral contraceptive consumption timing on substrate metabolism, cognition, and exercise performance in females: a randomised controlled trial.European journal of applied physiology · 2025Trial
- Lasting effects of oral contraceptives on fear responses to a safe context.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Article
- Associations between low sex hormone concentrations and depression in older women: An observational study.Maturitas · 2023Observational
- Striatal dopamine synthesis and cognitive flexibility differ between hormonal contraceptive users and nonusers.Cerebral cortex (New York, N.Y. : 1991) · 2023Article
- Article
- Morphologic alterations of the fear circuitry: the role of sex hormones and oral contraceptives.Frontiers in endocrinology · 2023Article
- SAR Study on Estrogen Receptor α/β Activity of (Iso)flavonoids: Importance of Prenylation, C-Ring (Un)Saturation, and Hydroxyl Substituents.Journal of agricultural and food chemistry · 2020Article
- A mutant form of ERα associated with estrogen insensitivity affects the coupling between ligand binding and coactivator recruitment.Science signaling · 2020Article
- Estrone Is a Strong Predictor of Circulating Estradiol in Women Age 70 Years and Older.The Journal of clinical endocrinology and metabolism · 2020Article
- Sex differences in schizophrenia, bipolar disorder, and post-traumatic stress disorder: Are gonadal hormones the link?British journal of pharmacology · 2019Review
- Steroid receptor/coactivator binding inhibitors: An update.Molecular and cellular endocrinology · 2019Review
- Article
- Structural underpinnings of oestrogen receptor mutations in endocrine therapy resistance.Nature reviews. Cancer · 2018Review
- Human-relevant potency threshold (HRPT) for ERα agonism.Archives of toxicology · 2018Article
- Structurally Novel Antiestrogens Elicit Differential Responses from Constitutively Active Mutant Estrogen Receptors in Breast Cancer Cells and Tumors.Cancer research · 2017Article
- ActivatingCancer discovery · 2017Article
- Article
- Cyclic Ketoximes as Estrogen Receptor β Selective Agonists.ChemMedChem · 2016Article
- Design of pathway preferential estrogens that provide beneficial metabolic and vascular effects without stimulating reproductive tissues.Science signaling · 2016Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The estrogen receptors, ERα and ERβ, are ligand-regulated transcription factors that control gene expression programs in target tissues. The molecular events underlying estrogen action involve minimally two steps, hormone binding to the ER ligand-binding domain followed by coactivator recruitment to the ER·ligand complex; this ligand·receptor·coactivator triple complex then alters gene expression. Conceptually, the potency of an estrogen in activating a cellular response should reflect the affinities that characterize both steps involved in the assembly of the active ligand·receptor·coactivator complex. Thus, to better understand the molecular basis of estrogen potency, we developed a completely in vitro system (using radiometric and time-resolved FRET assays) to quantify independently three parameters: (a) the affinity of ligand binding to ER, (b) the affinity of coactivator binding to the ER·ligand complex, and (c) the potency of ligand recruitment of coactivator. We used this system to characterize the binding and potency of 12 estrogens with both ERα and ERβ. Some ligands showed good correlations between ligand binding affinity, coactivator binding affinity, and coactivator recruitment potency with both ERs, whereas others showed correlations with only one ER subtype or displayed discordant coactivator recruitment potencies. When ligands with low receptor binding affinity but high coactivator recruitment potencies to ERβ were evaluated in cell-based assays, elevation of cellular coactivator levels significantly and selectively improved their potency. Collectively, our results indicate that some low affinity estrogens may elicit greater cellular responses in those target cells that express higher levels of specific coactivators capable of binding to their ER complexes with high affinity.
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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.