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)…

Induction of cytochrome P450 3A4 in primary human hepatocytes and activation of the human pregnane X receptor by tamoxifen and 4-hydroxytamoxifen

PB Desai, SC Nallani, RS Sane, LB Moore… - Drug metabolism and …, 2002 - ASPET
… antagonists or partial agonists of estrogen receptors, which are … antiestrogens activate
hPXR. In general, there was good agreement between the CYP3A4 induction and hPXR activation

… (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 …

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 …

Co-expression of drug metabolizing cytochrome P450 enzymes and estrogen receptor alpha (ESR1) in human liver: racial differences and the regulatory role of ESR1

JM Collins, D Wang - Drug metabolism and personalized therapy, 2021 - degruyter.com
… of estrogens is … -activated TF that regulates transcription of estrogen-responsive genes in
the cell nucleus [6]. However, ESR1 can also become activated in the absence of estrogen by …

Steroid regulation of drug-metabolizing cytochromes P450

K Monostory, Z Dvorak - Current drug metabolism, 2011 - ingentaconnect.com
… DNA sequence of the ERE, and transactivates gene expression in response to estrogens [60,
61]. Al… provides an explanation for their antiestrogenic properties, increased metabolism of …

CAR and PXR: the xenobiotic-sensing receptors

YE Timsit, M Negishi - Steroids, 2007 - Elsevier
… This is in contrast to the steroid nuclear receptors, the estrogen … (B) Crystal structure of the
ligand binding domain of hPXR (… This is important to prevent ER and GR from being activated

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. …