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: 2028.86   (req: < 5)

Gene RIFs: 287   (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: 2028.86   (req: >= 5)

Gene RIFs: 287   (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: 40

Tclin

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

Active Drugs: 5

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Expression Data (0 Tissues)

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No expression data found

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Target Illumination GWAS Analytics (TIGA)

TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.

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GENEVA

GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.

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GlyGen

GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.

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ARCHS4

ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.

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Approved Drugs (5)

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1 – 5 of 5

paclitaxel

NR1I2Tchem NR

INHIBITOR pEC50 : 8.05

droxidopa

NR1I2Tchem NR

AGONIST :

mifepristone

NR1I2Tchem NR

ANTAGONIST pKi : 8.74

linolenic acid

NR1I2Tchem NR

pKd : 8.56

dexamethasone

NR1I2Tchem NR

AGONIST pEC50 : 8.88

Active Ligands (40)

Explore Active Ligands

1 – 10 of 40

lithocholic acid

NR1I2Tchem NR

pIC50 : 7.74

Tularik

NR1I2Tchem NR

pKi : 7.29

guggulsterone

NR1I2Tchem NR

pKi : 7.41

5&beta;-pregnane-3,20-dione

NR1I2Tchem NR

pIC50 : 6.4

3-keto-lithocholic acid

NR1I2Tchem NR

: 6.54

hyperforin

NR1I2Tchem NR

pKi : 7.57

CHEMBL410683

NR1I2Tchem NR

pKi : 7.43

CHEMBL4209665

NR1I2Tchem NR

pEC50 : 7.8

CHEMBL2326845

NR1I2Tchem NR

pEC50 : 8

CHEMBL4217890

NR1I2Tchem NR

pEC50 : 7.26

Protein-Protein Interactions (168)

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1 – 10 of 168

• See Interactions on String-DB

CYP3A4

Tclin

Family:  Enzyme

Novelty:  0.00015515

Score:  0.962

Data Source:  STRINGDB

NCOA1

Tchem

Family:  Epigenetic

Novelty:  0.00344663

Score:  0.962

Data Source:  STRINGDB

RXRA

Tclin

Family:  NR

Novelty:  0.00244343

Score:  0.917

Data Source:  STRINGDB

NR0B2

Tchem

Family:  NR

Novelty:  0.0009861

Score:  0.881

Data Source:  STRINGDB

PPIG

Tchem

Family:  Enzyme

Novelty:  0.00014569

Score:  0.867

Data Source:  STRINGDB

CYP7A1

Tchem

Family:  Enzyme

Novelty:  0.00148194

Score:  0.859

Data Source:  STRINGDB

UGT1A1

Tchem

Family:  Enzyme

Novelty:  0.00135044

Score:  0.844

Data Source:  STRINGDB

ABCB1

Tchem

Family:  Transporter

Novelty:  0.00018144

Score:  0.843

Data Source:  STRINGDB

NCOR2

Tchem

Family:  TF

Novelty:  0.00066449

Score:  0.841

Data Source:  STRINGDB

EPRS

Tchem

Family:  Enzyme

Novelty:  0.00084896

Score:  0.836

Data Source:  STRINGDB

Nearest Tclin Targets

Nearest Tclin calculations are only available for targets with KEGG Pathway annotations.

Pathways (88)

Reactome (9)

WikiPathways (79)

Gene expression (Transcription) (R-HSA-74160)

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Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Gene expression (Transcription)	1452 targets	R-HSA-74160
Reactome	Generic Transcription Pathway	1195 targets	R-HSA-212436
Reactome	Metabolism of proteins	2050 targets	R-HSA-392499
Reactome	Nuclear Receptor transcription pathway	53 targets	R-HSA-383280
Reactome	Post-translational protein modification	1450 targets	R-HSA-597592

Name	Explore in Pharos	Explore in Source
Gene expression (Transcription)	1452 targets	R-HSA-74160
Generic Transcription Pathway	1195 targets	R-HSA-212436
Metabolism of proteins	2050 targets	R-HSA-392499
Nuclear Receptor transcription pathway	53 targets	R-HSA-383280
Post-translational protein modification	1450 targets	R-HSA-597592

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (29)

Functions (12)

Components (5)

Processes (12)

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10

1 – 10 of 12

GO Term	Evidence	Assigned by
DNA-binding transcription activator activity, RNA polymerase II-specific	Inferred from Direct Assay (IDA)	NTNU_SB
drug binding	Inferred from Direct Assay (IDA)	UniProtKB
nuclear receptor activity	Inferred from Direct Assay (IDA)	UniProtKB
RNA polymerase II regulatory region sequence-specific DNA binding	Inferred from Direct Assay (IDA)	NTNU_SB
nuclear receptor transcription coactivator activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
signaling receptor activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
transcription factor binding	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
transcription regulatory region sequence-specific DNA binding	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
DNA-binding transcription factor activity, RNA polymerase II-specific	Inferred from Sequence Alignment (ISA)	NTNU_SB
transcription coactivator activity	Traceable Author Statement (TAS)	ProtInc

Disease Associations ()

No disease associations found

GWAS Traits (6)

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1 – 5 of 6

GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
high density lipoprotein cholesterol measurement	EFO_0004612	4	2	4		74.1
apolipoprotein A 1 measurement	EFO_0004614	1	1	1		72.9
low density lipoprotein cholesterol measurement	EFO_0004611	1	1	1		52.7
lymphocyte percentage of leukocytes	EFO_0007993	1	1	1		50.6
total cholesterol measurement	EFO_0004574	1	1	1		42.3

• Explore on Target Illumination GWAS Analytics (TIGA)

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1 – 5 of 6

GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
high density lipoprotein cholesterol measurement	EFO_0004612	4		74.1
apolipoprotein A 1 measurement	EFO_0004614	1		72.9
low density lipoprotein cholesterol measurement	EFO_0004611	1		52.7
lymphocyte percentage of leukocytes	EFO_0007993	1		50.6
total cholesterol measurement	EFO_0004574	1		42.3

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UniProt Keyword Find Similar Targets

No Header	No Header
3D-structure
Activator
Alternative splicing
Complete proteome
DNA-binding
Metal-binding
Nucleus
Polymorphism
Receptor
Reference proteome

GWAS Trait Find Similar Targets

No Header	No Header
apolipoprotein A 1 measurement
C-reactive protein measurement
high density lipoprotein cholesterol measurement
low density lipoprotein cholesterol measurement
lymphocyte percentage of leukocytes
total cholesterol measurement

MGI Phenotype Find Similar Targets

No Header	No Header
behavior/neurological phenotype
cellular phenotype
homeostasis/metabolism phenotype
liver/biliary system phenotype

IDG Resources

No IDG generated resources found

Orthologs (11)

1 – 5 of 11

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	nuclear receptor subfamily 1 group I member 2	VGNC:7079	745458
Macaque	nuclear receptor subfamily 1 group I member 2		574226
Mouse	nuclear receptor subfamily 1, group I, member 2	MGI:1337040	18171
Rat	nuclear receptor subfamily 1, group I, member 2	RGD:69057	84385
Dog	nuclear receptor subfamily 1 group I member 2	VGNC:53079	403482

Species	Name	OMA	EggNOG	Inparanoid
Chimp	nuclear receptor subfamily 1 group I member 2
Macaque	nuclear receptor subfamily 1 group I member 2
Mouse	nuclear receptor subfamily 1, group I, member 2
Rat	nuclear receptor subfamily 1, group I, member 2
Dog	nuclear receptor subfamily 1 group I member 2

Publication Statistics

PubMed Score 2028.86

PubMed score by year

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PubTator Score 957.53

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Patents

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Related Publications

Text Mined References (322)

GeneRif Annotations (287)

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PMID	Year	Title