Nuclear Receptor Subfamily 1 Group I Member 2 (NR1I2) Human Recombinant Protein

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]

PXR: Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and isoflavones. Response to specific ligands is species-specific. Activated by naturally occurring steroids, such as pregnenolone and progesterone. Binds to a response element in the promoters of the CYP3A4 and ABCB1/MDR1 genes. Heterodimer with RXR. Interacts with NCOA1. Expressed in liver, colon and small intestine. Belongs to the nuclear hormone receptor family. NR1 subfamily. 7 isoforms of the human protein are produced by alternative splicing.

Protein type: DNA-binding; Nuclear receptor

Chromosomal Location of Human Ortholog: 3q12-q13.3

Cellular Component: nucleoplasm

Molecular Function: ligand-dependent nuclear receptor activity; protein binding; zinc ion binding; transcription coactivator activity; steroid hormone receptor activity; drug binding

Biological Process: steroid metabolic process; transcription initiation from RNA polymerase II promoter; intracellular receptor-mediated signaling pathway; positive regulation of transcription, DNA-dependent; xenobiotic metabolic process; drug export; exogenous drug catabolic process; xenobiotic transport; steroid hormone mediated signaling; positive regulation of transcription from RNA polymerase II promoter; gene expression; negative regulation of transcription, DNA-dependent; signal transduction