In the field of molecular biology, the pregnane X receptor (PXR), also known as the steroid and xenobiotic sensing nuclear receptor (SXR) or nuclear receptor subfamily 1, group I, member 2 (NR1I2) is a protein that in humans is encoded by the NR1I2 (nuclear Receptor subfamily 1, group I, member 2) gene.

Pregnane X receptor (PXR, NR1I2) is a prototypical member of the nuclear receptor superfamily. PXR can be activated by both endobiotics and xenobiotics. As a key xenobiotic receptor, the cellular function of PXR is mostly exerted by its binding to ...

Pregnane X receptor (PXR) is a nuclear receptor considered to be a master xenobiotic receptor that coordinately regulates the expression of genes encoding drug-metabolizing enzymes and drug transporters to essentially detoxify and eliminate xenobiotics and endotoxins from the body.

2002年4月1日 · Two closely related orphan nuclear hormone receptors — the pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) — have recently emerged as transcriptional regulators of...

PXR exerts its transcriptional regulation by binding to its DNA response elements as a heterodimer with the retinoid X receptor (RXR) and recruitment of a host of coactivators.

PXR shares a common NR modular structure with a conserved N-terminal DNA-binding domain (DBD) and a C-terminal ligand-binding domain (LBD). The DBD contains two zinc-finger motifs, which mediate interaction with specific DNA sequences known as …

We performed a cell-based high-throughput screen to identify PXR antagonists, using a library of approved and investigational drugs. Two approved drugs, pimecrolimus and pazopanib, emerged as novel potent antagonists of PXR activation, with IC 50 values of 1.2 and 4.1 µM, respectively.

Pregnane X receptor (PXR, NR1I2) is a prototypical member of the nuclear receptor superfamily. PXR can be activated by both endobiotics and xenobiotics. As a key xenobiotic receptor, the cellular function of PXR is mostly exerted by its binding to the regulatory gene sequences in a ligand-dependent …

2021年2月1日 · The pregnane X receptor (PXR) is a nuclear receptor which regulates drug metabolizing enzymes (DMEs) by activation from endogenous, as well as exogenous, ligands [1]. The most notable PXR controlled DME is the extremely abundant liver cytochrome P450 (CYP) 3A4, which accounts for the metabolism of an estimated 50% of clinically used drugs [2], [3].

Pregnane X receptor (PXR) is a nuclear receptor considered to be a master xenobiotic receptor that coordinately regulates the expression of genes encoding drug-metabolizing enzymes and drug transporters to essentially detoxify and eliminate xenobiotics and endotoxins from the body.