Estrogens and antiestrogens activate hPXR

W Mnif, JM Pascussi, A Pillon, A Escande, A Bartegi… - Toxicology letters, 2007 - Elsevier
… reevaluate estrogens for their ability to activate human PXR, we assayed estrogenic compounds
with two HeLa-derived reporter cell lines, the HGPXR cells, which detect hPXR ligands, …

[HTML][HTML] Biology of PXR: role in drug-hormone interactions

J Wang, S Dai, Y Guo, W Xie, Y Zhai - EXCLI journal, 2014 - ncbi.nlm.nih.gov
… sulfation, because sulfonated estrogens cannot bind to and activate ER, thus losing their …
Therefore hPXR activation would tip the hepatocellular androgen/estrogen balance toward …

Lignans, bacteriocides and organochlorine compounds activate the human pregnane X receptor (PXR)

MN Jacobs, GT Nolan, SR Hood - Toxicology and applied pharmacology, 2005 - Elsevier
… , activated hPXR by 26.6% and 17%, respectively. The pesticide trans-nonachlor activation
… Quercetin is believed to have a potent inhibitory effect upon estrogen sulfotransferase (EST)…

… (CAR) ligand binding domains from the human oestrogen receptor α (hERα) crystal structure, and the human peroxisome proliferator activated receptor α (PPARα) …

MN Jacobs, M Dickins, DFV Lewis - The Journal of steroid biochemistry and …, 2003 - Elsevier
… In order to understand the role of ligand in receptor activation molecular models of the
ERβ, hPXR, AhR and hCAR LBDs have been generated from a ligand bound hERα crystal …

Human pregnane X receptor is expressed in breast carcinomas, potential heterodimers formation between hPXR and RXR-alpha

I Conde, MVT Lobo, J Zamora, J Pérez, FJ González… - BMC cancer, 2008 - Springer
… in the mechanisms of resistance to antiestrogens (tamoxifen and … hPXR has been shown to
activate transcription of reporter … an interaction between estrogen action and RXR specifically …

CAR and PXR: xenosensors of endocrine disrupters?

XC Kretschmer, WS Baldwin - Chemico-biological interactions, 2005 - Elsevier
activate one or both receptors, including several endocrine disrupting chemicals. Environmental
estrogens, such … activate either PXR or both PXR and CAR. Because PXR and CAR are …

Elucidating the 'Jekyll and Hyde'nature of PXR: the case for discovering antagonists or allosteric antagonists

A Biswas, S Mani, MR Redinbo, MD Krasowski… - Pharmaceutical …, 2009 - Springer
… human PXR, which could also contribute estrogenic effects … Together, these data suggest
that estrogen could act through … (an environmental estrogen that also activates PXR and CYP …

A structural view of nuclear hormone receptor: endocrine disruptor interactions

A Le Maire, W Bourguet, P Balaguer - Cellular and molecular life sciences, 2010 - Springer
… Accordingly, current therapies of breast cancers are primarily based on estrogen
similar affinities or have similar potencies in activation of estrogen response element (ERE)-mediated …

The phytoestrogen coumestrol is a naturally occurring antagonist of the human pregnane X receptor

H Wang, H Li, LB Moore, MDL Johnson… - Molecular …, 2008 - academic.oup.com
… Disruption of the position of the terminal helix 12 in the LBD of the estrogen and estrogen-related
receptors is the molecular basis for the … Estrogens and antiestrogens activate hPXR. …

Disruption of Other Receptor Systems: Progesterone, Glucocorticoid and Mineralocorticoid Receptors, Peroxisome Proliferator-Activated Receptors, Pregnane X …

PD Darbre - Endocrine Disruption and Human Health, 2022 - Elsevier
… for its expression [2], it acts as a downstream effector of estrogen signaling. In addition to …
, the antiestrogen tamoxifen, and the component of the contraceptive pill ethinyl estradiol. …