Pregnane X Receptor (PXR) Polymorphisms and Cancer Treatment [PDF]
Biomolecules, 2021 Pregnane X Receptor (PXR) belongs to the nuclear receptors’ superfamily and mainly functions as a xenobiotic sensor activated by a variety of ligands. PXR is widely expressed in normal and malignant tissues. Drug metabolizing enzymes and transporters are
Aikaterini Skandalaki +2 more
doaj +8 more sources
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
Marine Ligands of the Pregnane X Receptor (PXR): An Overview [PDF]
Marine Drugs, 2019 Pregnane X Receptor (PXR) is a ligand-activated transcription factor which binds many structurally different molecules. The receptor is able to regulate the expression of a wide array of genes and is involved in cancer and different key physiological ...
Alejandro Carazo +2 more
doaj +6 more sources
Discrepancy in interactions and conformational dynamics of pregnane X receptor (PXR) bound to an agonist and a novel competitive antagonist [PDF]
Computational and Structural Biotechnology Journal, 2022 Pregnane X receptor (PXR) is a nuclear receptor with an essential role in regulating drug metabolism genes. While the mechanism of action for ligand-mediated PXR agonism is well-examined, its ligand-mediated inhibition or antagonism is poorly understood.
Azam Rashidian +6 more
doaj +5 more sources
Pregnane X receptor (PXR)-mediated gene repression and cross-talk of PXR with other nuclear receptors via coactivator interactions [PDF]
Frontiers in Pharmacology, 2016 Pregnane X receptor is a ligand-activated nuclear receptor that mainly controls inducible expression of xenobiotics handling genes including biotransformation enzymes and drug transporters.
Petr Pavek
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The 3ʹ-untranslated region contributes to the pregnane X receptor (PXR) expression down-regulation by PXR ligands and up-regulation by glucocorticoids [PDF]
Acta Pharmaceutica Sinica B, 2020 Pregnane X receptor (PXR) is the major regulator of xenobiotic metabolism. PXR itself is controlled by various signaling molecules including glucocorticoids. Moreover, negative feed-back regulation has been proposed at the transcriptional level.
Tomas Smutny +7 more
doaj +4 more sources
Allosteric Antagonism of the Pregnane X Receptor (PXR): Current-State-of-the-Art and Prediction of Novel Allosteric Sites [PDF]
Cells, 2022 The pregnane X receptor (PXR, NR1I2) is a xenobiotic-activated transcription factor with high levels of expression in the liver. It not only plays a key role in drug metabolism and elimination, but also promotes tumor growth, drug resistance, and ...
Rajamanikkam Kamaraj +2 more
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Resveratrol as an Inhibitor of Pregnane X Receptor (PXR): Another Lesson in PXR Antagonism
Journal of Pharmacological Sciences, 2014 .: The pregnane X receptor (PXR) plays a central role in the regulation of metabolism. Only few PXR antagonists have been described and the mechanism of PXR inhibition is mostly hypothetical or believed to be allosteric.
Tomas Smutny, Petr Pavek
doaj +6 more sources
High Pregnane X Receptor (PXR) Expression Is Correlated with Poor Prognosis in Invasive Breast Carcinoma. [PDF]
Diagnostics (Basel), 2021 Pregnane X Receptor (PXR) is involved in human cancer, either by directly affecting carcinogenesis or by inducing drug-drug interactions and chemotherapy resistance.
Theocharis S +11 more
europepmc +7 more sources
Mathematical Models in the Description of Pregnane X Receptor (PXR)-Regulated Cytochrome P450 Enzyme Induction. [PDF]
Int J Mol Sci, 2018 The pregnane X receptor (PXR) is a drug/xenobiotic-activated transcription factor of crucial importance for major cytochrome P450 xenobiotic-metabolizing enzymes (CYP) expression and regulation in the liver and the intestine.
Tebbens JD +4 more
europepmc +5 more sources