ArticleThe Journal of biological chemistry2021
Bisphenol A derivatives act as novel coactivator-binding inhibitors for estrogen receptor β.
Article in The Journal of biological chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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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
11 citing papers in PubMed, 29 citations in OpenAlex.
- Replacing BPA: Structural Substitutes BPAF Binding to the Progesterone Receptor Elevates Breast Cancer Risk.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Migration of Bisphenol A and Its Derivatives From Epoxy Coatings and Demand for BPA-NI Products: Scientific Insights and Perspectives Leading to Regulation (EU) 2024/3190.Chemistry, an Asian journal · 2025Review
- Toxic Effects of BPAF on Marine Medaka (Toxics · 2025Article
- Loss of adult visual responses by developmental BPA exposure is correlated with altered estrogenic signaling.Communications biology · 2025Article
- The Influence of Bisphenol A on the Molecular Biological Characteristics of Human Colon Adenocarcinoma HT-29 Culture Cells.Bulletin of experimental biology and medicine · 2025Article
- Zooming into Gene Activation: Estrogen Receptor α Dimerization and DNA Binding Visualized by High-Speed Atomic Force Microscopy.ACS nano · 2025Article
- Article
- Invisible Hand behind Female Reproductive Disorders: Bisphenols, Recent Evidence and Future Perspectives.Toxics · 2023Review
- NTS, NTSR1 and ERs in the Pituitary-Gonadal Axis of Cycling and Postnatal Female Rats after BPA Treatment.International journal of molecular sciences · 2023Article
- Article
- The Association between the Bisphenols Residues in Amniotic Fluid and Fetal Abnormalities in Polish Pregnant Women-Its Potential Clinical Application.International journal of molecular sciences · 2023Article
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 2 countries.
Funding
Abstract
Bisphenol A and its derivatives are recognized as endocrine disruptors based on their complex effects on estrogen receptor (ER) signaling. While the effects of bisphenol derivatives on ERα have been thoroughly evaluated, how these chemicals affect ERβ signaling is less well understood. Herein, we sought to identify novel ERβ ligands using a radioligand competitive binding assay to screen a chemical library of bisphenol derivatives. Many of the compounds identified showed intriguing dual activities as both ERα agonists and ERβ antagonists. Docking simulations of these compounds and ERβ suggested that they bound not only to the canonical binding site of ERβ but also to the coactivator binding site located on the surface of the receptor, suggesting that they act as coactivator-binding inhibitors (CBIs). Receptor-ligand binding experiments using WT and mutated ERβ support the presence of a second ligand-interaction position at the coactivator-binding site in ERβ, and direct binding experiments of ERβ and a coactivator peptide confirmed that these compounds act as CBIs. Our study is the first to propose that bisphenol derivatives act as CBIs, presenting critical insight for the future development of ER signaling-based drugs and their potential to function as endocrine disruptors.
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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.