ArticleEnvironmental health perspectives2012
Bisphenol A and its analogues activate human pregnane X receptor.
Article in Environmental health perspectives, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 64 papers.
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Who cites it
64 citing papers in PubMed, 197 citations in OpenAlex.
- A Universal Plasticizer Alkylsulfonic Phenyl Ester Activates Pregnane X Receptor to Increase Intestinal Cholesterol Uptake.International journal of molecular sciences · 2026Article
- Emerging evidence for skeletal muscle as a target of BPA exposure.BMC endocrine disorders · 2026Review
- Bisphenol F and Steatotic Liver Disease: Resolving the PXR Paradox Through Stress Pathway Mechanisms.Biomedicines · 2025Review
- Insights into the Imprinting and Rebinding Performance of Molecularly Imprinted Hybrids for Bisphenol A and Bisphenol F.ACS applied materials & interfaces · 2025Article
- Interaction of Bisphenol A and Its Analogs with Estrogen and Androgen Receptor from Atlantic Cod (Environmental science & technology · 2024Article
- An insight into carcinogenic activity and molecular mechanisms of Bis(2-ethylhexyl) phthalate.Frontiers in toxicology · 2024Article
- Cannabidiol promotes intestinal cholesterol uptake mediated by Pregnane X receptor.Frontiers in endocrinology · 2024Article
- A review on immunomodulatory effects of BPA analogues.Archives of toxicology · 2023Review
- Are BPA Substitutes as Obesogenic as BPA?International journal of molecular sciences · 2022Review
- Pregnane X Receptor and the Gut-Liver Axis: A Recent Update.Drug metabolism and disposition: the biological fate of chemicals · 2022Review
- Article
- Effects of Dicyclohexyl Phthalate Exposure on PXR Activation and Lipid Homeostasis in Mice.Environmental health perspectives · 2021Article
- Key Characteristics of Cardiovascular Toxicants.Environmental health perspectives · 2021Article
- Endocrine-Disrupting Chemicals and Vitamin D Deficiency in the Pathogenesis of Uterine Fibroids.Journal of advanced pharmacy research · 2021Article
- Human exposure of bisphenol A and its analogues: understandings from human urinary excretion data and wastewater-based epidemiology.Environmental science and pollution research international · 2020Article
- Discovery of novel oestrogen receptor α agonists and antagonists by screening a revisited privileged structure moiety for nuclear receptors.Scientific reports · 2019Article
- Evolutionary Plasticity in Detoxification Gene Modules: The Preservation and Loss of the Pregnane X Receptor in Chondrichthyes Lineages.International journal of molecular sciences · 2019Article
- Exploring the PXR ligand binding mechanism with advanced Molecular Dynamics methods.Scientific reports · 2018Article
- Crosstalk between BPA and FXRα Signaling Pathways Lead to Alterations of Undifferentiated Germ Cell Homeostasis and Male Fertility Disorders.Stem cell reports · 2018Article
- Activating the pregnane X receptor by imperatorin attenuates dextran sulphate sodium-induced colitis in mice.British journal of pharmacology · 2018Article
4 more citing papers are in PubMed but not listed here.
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
backgroundBisphenol A (BPA) is a base chemical used extensively in many consumer products. BPA and its analogues are present in environmental and human samples. Many endocrine-disrupting chemicals, including BPA, have been shown to activate the pregnane X receptor (PXR), a nuclear receptor that functions as a master regulator of xenobiotic metabolism. However, the detailed mechanism by which these chemicals activate PXR remains unknown.
objectiveWe investigated the mechanism by which BPA interacts with and activates PXR and examined selected BPA analogues to determine whether they bind to and activate PXR.
methodsCell-based reporter assays, in silico ligand-PXR docking studies, and site-directed mutagenesis were combined to study the interaction between BPA and PXR. We also investigated the influence of BPA and its analogues on the regulation of PXR target genes in human LS180 cells.
resultsWe found that BPA and several of its analogues are potent agonists for human PXR (hPXR) but do not affect mouse PXR activity. We identified key residues within hPXR's ligand-binding pocket that constitute points of interaction with BPA. We also deduced the structural requirements of BPA analogues that activate hPXR. BPA and its analogues can also induce PXR target gene expression in human LS180 cells.
conclusionsThe present study advances our understanding of the mechanism by which BPA interacts with and activates human PXR. Activation of PXR by BPA may explain some of the adverse effects of BPA in humans.
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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.