The Anti-Cancer Drug Dabrafenib Is a Potent Activator of the Human Pregnane X Receptor
The human pregnane X receptor (hPXR) is activated by a large set of endogenous and exogenous compounds and plays a critical role in the control of detoxifying enzymes and transporters regulating liver and gastrointestinal drug metabolism and clearance ...
N. Creusot+14 more
semanticscholar +1 more source
Pregnane X receptor and human malignancy.
Pregnane X Receptor (PXR) is a member of the nuclear receptor superfamily, expressed in liver, intestine and other tissues. PXR exerts transcriptional regulation by binding to its DNA response elements as an heterodimer with Retinoid X Receptor (RXR).
Stamatios Theocharis+2 more
openaire +4 more sources
Promoter DNA methylation of farnesoid X receptor and pregnane X receptor modulates the intrahepatic cholestasis of pregnancy phenotype. [PDF]
The intrahepatic cholestasis of pregnancy (ICP) is a multifactorial liver disorder which pathogenesis involves the interplay among abnormal bile acid (BA) levels, sex hormones, environmental factors, and genetic susceptibility.
Romina Cabrerizo+7 more
doaj +1 more source
The pregnane X receptor: from bench to bedside [PDF]
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 ...
Xiaochao Ma+2 more
openaire +3 more sources
Spectroscopic, Structural, and Theoretical Studies of Halide Complexes with a Urea-based Tripodal Receptor [PDF]
A urea-based tripodal receptor L substituted with p-cyanophenyl groups has been studied for halide anions by $^1$H NMR spectroscopy, density functional theory (DFT) calculations and X-ray crystallography. The $^1$H NMR titration studies suggest that the receptor forms a 1:1 complex with an anion, showing the binding trend in the order of fluoride ...
arxiv +1 more source
Revising Berg-Purcell for finite receptor kinetics [PDF]
From nutrient uptake, to chemoreception, to synaptic transmission, many systems in cell biology depend on molecules diffusing and binding to membrane receptors. Mathematical analysis of such systems often neglects the fact that receptors process molecules at finite kinetic rates.
arxiv +1 more source
The pregnane X receptor (PXR), or nuclear receptor (NR) 1I2, is a ligand-activated NR superfamily member that is enriched in liver and intestine in mammals.
Wenqi Cui+5 more
semanticscholar +1 more source
Hepatic ZBTB22-mediated detoxification ameliorates acetaminophen-induced liver injury by inhibiting pregnane X receptor signaling. [PDF]
Summary: Overdose acetaminophen (APAP) can cause acute liver injury (ALI), but the underlying mechanism remains undetermined. This study explored the role of hepatic Zinc Finger And BTB Domain Containing 22 (ZBTB22) in defense against APAP-mediated ...
Chen Y+13 more
europepmc +2 more sources
Constitutive androstane receptor and pregnane X receptor genotype influence efavirenz plasma concentration and CYP2B6 enzyme activity. [PDF]
Efavirenz is metabolized by CYP2B6, an inducible enzyme whose expression is regulated by the constitutive androstane receptor and pregnane X receptor nuclear receptors. CAR and PXR are encoded by genetically polymorphic NR1I2 and NR1I3, respectively.
Petros Z+3 more
europepmc +2 more sources
Modulation of Xenobiotic Receptors by Steroids
Nuclear receptors (NRs) are ligand-activated transcription factors that regulate the expression of their target genes. NRs play important roles in many human diseases, including metabolic diseases and cancer, and are therefore a key class of therapeutic ...
Delira Robbins+2 more
doaj +1 more source