The pregnane X receptor (PXR, NR1I2) is a nuclear receptor which exerts its regulatory function by heterodimerization with the retinoid-X-receptor α (RXRα, NR2B1) and binding to the promoter and enhancer regions of diverse target genes.
Juan Pablo Rigalli +3 more
doaj +1 more source
A novel panel of mouse models to evaluate the role of human pregnane X receptor and constitutive androstane receptor in drug response [PDF]
The pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) are closely related orphan nuclear hormone receptors that play a critical role as xenobiotic sensors in mammals.
Zevnik, Branko +13 more
core +1 more source
Resveratrol as an Inhibitor of Pregnane X Receptor (PXR): Another Lesson in PXR Antagonism
.: 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 +1 more source
The evolution of drug-activated nuclear receptors: one ancestral gene diverged into two xenosensor genes in mammals [PDF]
BACKGROUND: Drugs and other xenobiotics alter gene expression of cytochromes P450 (CYP) by activating the pregnane X receptor (PXR) and constitutive androstane receptor (CAR) in mammals.
Urs A Meyer +26 more
core +1 more source
Activation of Human Stearoyl-Coenzyme A Desaturase 1 Contributes to the Lipogenic Effect of PXR in HepG2 Cells [PDF]
The pregnane X receptor (PXR) was previously known as a xenobiotic receptor. Several recent studies suggested that PXR also played an important role in lipid homeostasis but the underlying mechanism remains to be clearly defined.
Wei, Yijuan +23 more
core +1 more source
Targeting the pregnane X receptor in liver injury [PDF]
The nuclear receptor pregnane X receptor (PXR) is a well-characterized hepatic xenobiotic sensor whose activation by chemically diverse compounds results in the induction of drug clearance pathways that rid the body of potentially toxic substances, thus conferring protection from foreign chemicals and endobiotics.PXR activities are implicated in drug ...
Tao, Li +5 more
openaire +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
Role of pregnane X receptor in chemotherapeutic treatment [PDF]
Pregnane X receptor (PXR) is a member of the nuclear receptor superfamily that differently expresses not only in human normal tissues but also in numerous types of human cancers. PXR can be activated by many endogenous substances and exogenous chemicals, and thus affects chemotherapeutic effects and intervenes drug-drug interactions by regulating its ...
Wei, Zhuo +5 more
openaire +2 more sources
A Fresh Insight into the Interaction of Natural Products with Pregnane X Receptor
The discovery that various drugs (e.g., phenobarbital) stimulate their own metabolism through a mechanism coined as enzymatic induction opened up a fascinating road that eventually led to the accurate biochemical characterization of the pregnane X ...
Salvador Máñez
doaj +1 more source
Flame model Pregnane X receptor activation
Dataset containing a Flame QSAR model for predicting Pregnane X receptor activation. The model is described in the metadata.txt file. The PXR_FAIR.tgz file can be imported into any instance of the open-source Flame (https://github.com/phi-grib/flame) and
Pastor, Manuel
core +1 more source

