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The role of pregnane X receptor (PXR) in substance metabolism [PDF]
Frontiers in Endocrinology, 2022 As a member of the nuclear receptor (NR) superfamily, pregnane X receptor (PXR; NR1I2) is a ligand-activated transcription factor that plays a crucial role in the metabolism of xenobiotics and endobiotics in mammals.
Ye Lv +7 more
doaj +6 more sources
The Interface between Cell Signaling Pathways and Pregnane X Receptor [PDF]
Cells, 2021 Highly expressed in the enterohepatic system, pregnane X receptor (PXR, NR1I2) is a well-characterized nuclear receptor (NR) that regulates the expression of genes in the liver and intestines that encode key drug metabolizing enzymes and drug transporter
Robert S. Rogers +14 more
doaj +4 more sources
Pregnane X Receptor‒4β‐Hydroxycholesterol Axis in the Regulation of Overweight‐ and Obesity‐Induced Hypertension [PDF]
Journal of the American Heart Association: Cardiovascular and Cerebrovascular Disease, 2022 Background Mechanisms mediating hypertensive effects of overweight and obesity have not been fully elucidated. We showed previously that activation of pregnane X receptor (PXR) by rifampicin elevates 24‐hour blood pressure (BP) and plasma 4β ...
Roosa Rahunen +6 more
doaj +4 more sources
Cannabidiol promotes intestinal cholesterol uptake mediated by Pregnane X receptor [PDF]
Frontiers in EndocrinologyBackgroundCannabidiol (CBD), a non-psychoactive phytocannabinoid of cannabis, is therapeutically used as an analgesic, anti-convulsant, anti-inflammatory, and anti-psychotic drug.
Conner Brown +4 more
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Evolution of pharmacologic specificity in the pregnane X receptor [PDF]
BMC Evolutionary Biology, 2008 Background The pregnane X receptor (PXR) shows the highest degree of cross-species sequence diversity of any of the vertebrate nuclear hormone receptors. In this study, we determined the pharmacophores for activation of human, mouse, rat, rabbit, chicken,
Reschly Erica J +3 more
doaj +3 more sources
Targeting the pregnane X receptor using microbial metabolite mimicry
EMBO Molecular Medicine, 2020 The human PXR (pregnane X receptor), a master regulator of drug metabolism, has essential roles in intestinal homeostasis and abrogating inflammation. Existing PXR ligands have substantial off‐target toxicity.
Zdeněk Dvořák +41 more
doaj +2 more sources
The pregnane X receptor: from bench to bedside [PDF]
Expert Opinion on Drug Metabolism and Toxicology, 2008 The pregnane X receptor (PXR; NR1I2), a member of the nuclear receptor superfamily, regulates the expression of metabolic enzymes and transporters involved in the response of mammals to their chemical environment.To summarize the functions and clinical implications of PXR.In the current review, the clinical implications of PXR are discussed, and the ...
Jeffrey R Idle, Frank J Gonzalez
exaly +3 more sources
Forsythiaside A Reduces Acetaminophen Hepatotoxic Metabolism by Inhibiting Pregnane X Receptor [PDF]
MoleculesOverdose intake of acetaminophen (APAP) causes liver injury involving hepatic drug metabolism and activation of oxidative stress pathways, and forsythiaside A (FA) has hepatoprotective pharmacological activity, but knowledge of the mechanism of FA ...
Sisi Pu +6 more
doaj +2 more sources
Associations between Pregnane X Receptor and Breast Cancer Growth and Progression
Cells, 2020 Pregnane X receptor (PXR, NR1I2) is a member of the ligand-activated nuclear receptor superfamily. This receptor is promiscuous in its activation profile and is responsive to a broad array of both endobiotic and xenobiotic ligands.
Bradley A. Creamer +7 more
doaj +3 more sources
SPA70 is a potent antagonist of human pregnane X receptor [PDF]
Nature Communications, 2017 The xenobiotic-activated human pregnane X receptor (hPXR) regulates drug metabolism. Here the authors develop hPXR modulators, which are of potential therapeutic interest and functionally and structurally characterize the antagonist SPA70 and the ...
Wenwei Lin +9 more
doaj +3 more sources