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GoPubMed Proteins lists recent and important papers and reviews for proteins. Page last changed on 19 Aug 2016.

Nuclear receptor subfamily 1, group I, member 2

SAR, pregnane X receptor
This gene product belongs to the nuclear receptor superfamily, members of which are transcription factors characterized by a ligand-binding domain and a DNA-binding domain. The encoded protein is a transcriptional regulator of the cytochrome P450 gene CYP3A4, binding to the response element of the CYP3A4 promoter as a heterodimer with the 9-cis retinoic acid receptor RXR. It is activated by a range of compounds that induce CYP3A4, including dexamethasone and rifampicin. Several alternatively spliced transcripts encoding different isoforms, some of which use non-AUG (CUG) translation initiation codon, have been described for this gene. Additional transcript variants exist, however, they have not been fully characterized. [provided by RefSeq, Jul 2008] (from NCBI)
Top mentioned proteins: CAN, ACID, V1a, CYP3A4, HAD
Papers on SAR
Structure-Activity Studies of Bis-O-Arylglycolamides: Inhibitors of the Integrated Stress Response.
New
Renslo et al., San Francisco, United States. In Chemmedchem, Feb 2016
Herein we describe structure-activity relationship (SAR) studies of bis-O-arylglycolamides, first-in-class integrated stress response inhibitors (ISRIB).
Nuclear receptors and drug metabolism for the personalization of cancer therapy.
New
Toffoli et al., Italy. In Expert Opin Drug Metab Toxicol, Feb 2016
The study of the host genetic background of Pregnane X Receptor (PXR; NR1I2) and Constitutive Androstane Receptor (CAR; NR1I3 and NR1I4), represents a new and attractive strategy to discern variability in ADME of antineoplastic drugs.
From Sphingosine Kinase to Dihydroceramide Desaturase: A Structure-Activity Relationship (SAR) Study of the Enzyme Inhibitory and Anticancer Activity of 4-((4-(4-chlorophenyl)thiazol-2-ylamino)phenol (SKI-II).
New
Flynn et al., In J Med Chem, Feb 2016
In this study we have delineated the structure-activity relationship (SAR) for these different targets and correlated them to that required for anticancer activity and determined that Des1 inhibition is primarily responsible for the antiproliferative effects of SKI-II and its analogues.
Cross-talk between EPAS-1/HIF-2α and PXR Signaling Pathway Regulates Multi-drug Resistance of Stomach Cancer Cell.
New
Xu et al., Beijing, China. In Int J Biochem Cell Biol, Feb 2016
Our results revealed that EPAS-1 interacts with Pregnane X Receptor (PXR), a nuclear receptor that regulates multiple genes' transcription involved in multi-drugs resistance (MDR) process.
Review article: the potential mechanisms of action of rifaximin in the management of inflammatory bowel diseases.
Review
New
Sartor, Chapel Hill, United States. In Aliment Pharmacol Ther, Jan 2016
In experimental colitis models, rifaximin antagonised the effects of tumour necrosis factor-α on intestinal epithelial cells by activating pregnane X receptor, which inhibits nuclear factor-κB-mediated proinflammatory mediators and induces detoxification genes (e.g.
Pharmacology of bile acid receptors: Evolution of bile acids from simple detergents to complex signaling molecules.
Review
New
Li et al., East Lansing, United States. In Pharmacol Res, Jan 2016
Ultimately, seminal studies by many investigators led to the discovery of several bile acid-activated receptors including the farnesoid X receptor, the vitamin D receptor, the pregnane X receptor, TGR5, α5 β1 integrin, and sphingosine-1-phosphate receptor 2. Several of these receptors are expressed outside of the gastrointestinal system, indicating that bile acids may have diverse functions throughout the body.
SUMOylation of pregnane X receptor suppresses rifampicin-induced CYP3A4 and P-gp expression and activity in LS174T cells.
New
Bi et al., Guangzhou, China. In J Pharmacol Sci, Jan 2016
UNASSIGNED: The pregnane X receptor (PXR) has been well-established as a critical mediator in regulating important drug metabolizing enzymes and transporter proteins, including cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp).
Mobile Phone Radiation: Physiological & Pathophysiologcal Considerations.
Review
New
K Sri, In Indian J Physiol Pharmacol, Apr 2015
For the mobile phones, ICNIRP 1998 guidelines restrict spatial peak of microwave exposure to 2 W/Kg SAR values averaged over 10 g of tissue for 6 minutes.
Pathogenesis and Management of Pruritus in PBC and PSC.
Review
Beuers et al., In Dig Dis, 2014
The current guideline-based recommendations include the anion exchange resins colestyramine, the pregnane X receptor-agonist and enzyme inducer rifampicin, the μ-opioid antagonist naltrexone, and the selective serotonin reuptake inhibitors sertraline.
Update on SAR Studies Toward New COX-1 Selective Inhibitors.
Review
Perrone et al., Bari, Italy. In Curr Med Chem, 2014
New selective inhibitors were very often discovered as a minor achievement during SAR investigations to discover selective COX-2 inhibitors (COXIBs).
Bile acid signaling in metabolic disease and drug therapy.
Review
Impact
Chiang et al., Tokelau. In Pharmacol Rev, 2014
The bile acid-activated nuclear receptors farnesoid X receptor, pregnane X receptor, constitutive androstane receptor, vitamin D receptor, and G protein-coupled bile acid receptor play critical roles in the regulation of lipid, glucose, and energy metabolism, inflammation, and drug metabolism and detoxification.
Symbiotic bacterial metabolites regulate gastrointestinal barrier function via the xenobiotic sensor PXR and Toll-like receptor 4.
Impact
Mani et al., United States. In Immunity, 2014
Here we showed that microbial-specific indoles regulated intestinal barrier function through the xenobiotic sensor, pregnane X receptor (PXR).
Naturally occurring sulfonium-ion glucosidase inhibitors and their derivatives: a promising class of potential antidiabetic agents.
Review
Impact
Pinto et al., Canada. In Acc Chem Res, 2014
Through structure-activity relationship (SAR) studies, we have modified the natural compounds to derive more potent, nanomolar inhibitors of human MGAM and SI.
Human PXR modulates hepatotoxicity associated with rifampicin and isoniazid co-therapy.
Impact
Ma et al., Kansas City, United States. In Nat Med, 2013
Here, using a pregnane X receptor (PXR)-humanized mouse model, we found that co-treatment with RIF and INH causes accumulation of the endogenous hepatotoxin protoporphyrin IX in the liver through PXR-mediated alteration of the heme biosynthesis pathway.
Systemic acquired resistance: turning local infection into global defense.
Review
Impact
Dong et al., Durham, United States. In Annu Rev Plant Biol, 2012
Systemic acquired resistance (SAR) is an induced immune mechanism in plants.
Human pregnane X receptor genotype of the donor but not of the recipient is a risk factor for delayed graft function after renal transplantation.
GeneRIF
Schaeffeler et al., Frankfurt am Main, Germany. In Clin Pharmacol Ther, 2012
PXR may be associated with risk of Delayed graft function (DGF), independent of previously identified risk factors.
4-Methylenesterols from Theonella swinhoei sponge are natural pregnane-X-receptor agonists and farnesoid-X-receptor antagonists that modulate innate immunity.
GeneRIF
Zampella et al., Napoli, Italy. In Steroids, 2012
Results provide a way to development of a dual PXR agonist/FXR antagonist with a robust immunomodulatory activity and endowed with the ability to modulate the expression of bile acid-regulated genes in the liver.
Pregnane X receptor regulates drug metabolism and transport in the vasculature and protects from oxidative stress.
GeneRIF
Bishop-Bailey et al., Guildford, United Kingdom. In Cardiovasc Res, 2012
Pregnane X receptor regulates drug metabolism and transport in the vasculature and protects from oxidative stress.
Rifampicin-independent interactions between the pregnane X receptor ligand binding domain and peptide fragments of coactivator and corepressor proteins.
GeneRIF
Thompson et al., Chapel Hill, United States. In Biochemistry, 2012
The mechanism of ligand-dependent activation in pregnane X receptor differs significantly from that seen in many other nuclear receptors.
Pregnane X receptor and yin yang 1 contribute to the differential tissue expression and induction of CYP3A5 and CYP3A4.
GeneRIF
Wojnowski et al., Mainz, Germany. In Plos One, 2011
Pregnane X receptor and yin yang 1 contribute to the differential tissue expression and induction of CYP3A5 and CYP3A4.
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