Results 1 to 10 of about 6,697 (112)
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 also under PXR’s regulation. Antineoplastic agents are of particular interest since cancer patients
Skandalaki A, Sarantis P, Theocharis S.
europepmc +7 more sources
The role of pregnane X receptor (PXR) in substance metabolism. [PDF]
Front Endocrinol (Lausanne), 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. The tissue distribution of PXR is parallel to its function with high expression in the liver and small intestine and moderate expression ...
Lv Y +5 more
europepmc +4 more sources
Marine Ligands of the Pregnane X Receptor (PXR): An Overview. [PDF]
Mar 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 processes such as the metabolism of drugs/xenobiotics and endogenous compounds including lipids and ...
Carazo A, Mladěnka P, Pávek P.
europepmc +5 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. The clinical significance of PXR expression in invasive breast carcinoma was evaluated in the present study.
Theocharis S +11 more
europepmc +5 more sources
Pregnane X Receptor (PXR)-Mediated Gene Repression and Cross-Talk of PXR with Other Nuclear Receptors via Coactivator Interactions. [PDF]
Front Pharmacol, 2016 Pregnane X receptor is a ligand-activated nuclear receptor (NR) that mainly controls inducible expression of xenobiotics handling genes including biotransformation enzymes and drug transporters. Nowadays it is clear that PXR is also involved in regulation of intermediate metabolism through trans-activation and trans-repression of genes controlling ...
Pavek P.
europepmc +5 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. One of the major target genes regulated by PXR is the cytochrome P450 enzyme (CYP3A4), which is the most important human drug ...
Tebbens JD +4 more
europepmc +4 more sources
Metformin suppresses pregnane X receptor (PXR)-regulated transactivation of CYP3A4 gene [PDF]
Biochemical Pharmacology, 2011 Metformin is widely used in the treatment of type-2 diabetes. The pleotropic effects of metformin on glucose and lipid metabolism have been proposed to be mediated by the activation of AMP-activated protein kinase (AMPK) and the subsequent up-regulation of small heterodimer partner (SHP).
Lucie, Krausova +6 more
openaire +2 more sources
Correlation of High-Throughput Pregnane X Receptor (PXR) Transactivation and Binding Assays [PDF]
SLAS Discovery, 2004 Pregnane X receptor (PXR) transactivation and binding assays have been developed into high-throughput assays, which are robust and reproducible (Z' > 0.5). For most compounds, there was a good correlation between the results of the transactivation and binding assays.
Zhengrong, Zhu +12 more
openaire +2 more sources
Regulation of a xenobiotic sulfonation cascade by nuclear pregnane X receptor (PXR) [PDF]
Proceedings of the National Academy of Sciences, 2002 The nuclear receptor PXR (pregnane X receptor) protects the body from hepatotoxicity of secondary bile acids such as lithocholic acid (LCA) by inducing expression of the hydroxylating cytochrome P450 enzyme CYP3A and promoting detoxification. We found that activation of PXR also increases the activity and gene expression of the phase II conjugating ...
Junichiro, Sonoda +5 more
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Pregnane X receptor (PXR) protects against cisplatin-induced acute kidney injury in mice
Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease, 2021 Cisplatin-induced acute kidney injury (CAKI) has been recognized as one of the most serious side effects of cisplatin. Pregnane X receptor (PXR) is a ligand-dependent nuclear receptor and serves as a master regulator of xenobiotic detoxification.
Zhilin, Luan +13 more
openaire +2 more sources