Tchem NR1I2 Nuclear receptor subfamily 1 group I member 2

Protein Summary

Description

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. 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]

Uniprot Accession IDs

• O75469
• Q006P5
• Q008C8
• Q96AC7
• Q9UJ22
• Q9UJ23
• Q9UJ24
• Q9UJ25
• Q9UJ26
• Q9UJ27
• Q9UNW4

Gene Name

• NR1I2

Ensembl ID

• ENST00000337940
• ENSP00000336528
• ENSG00000144852
• ENST00000638727
• ENSP00000492264
• ENST00000640105
• ENSP00000492881

Symbol

• PXR
• BXR
• PAR
• PRR
• PXR
• SAR
• SXR
• ONR1
• PAR1
• PAR2
• PARq

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
chemical	1
co-expressed gene	1
molecular function	0.97
biological term	0.8
biological process	0.73

Protein Classes

PANTHER Classes

Protein / Transcription Factor / Nuclear Receptor Subfamily 1 Group I Member 2

Protein / Receptor / Nuclear Receptor Subfamily 1 Group I Member 2

Protein / Nucleic Acid Binding / Nuclear Receptor Subfamily 1 Group I Member 2

Protein / ... / C4 Zinc Finger Nuclear Receptor / Nuclear Receptor Subfamily 1 Group I Member 2

DTO Classes

Protein / Nuclear Receptor / Vitamin D Receptor-like Receptors / Nuclear Receptor Subfamily 1 Group I Member 2

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 2265.46   (req: < 5)

Gene RIFs: 336   (req: <= 3)

Antibodies: 380   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 2265.46   (req: >= 5)

Gene RIFs: 336   (req: > 3)

Antibodies: 380   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 24

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 46

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 5