Aliases
BXR; PAR; PRR; PXR; SAR; SXR; ONR1; PAR1; PAR2; PARq
NRR Pathway
Summary
(From RefSeq)
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]
Function
(From Aceview)
There are�138 articles�specifically referring to this gene in PubMed. Functionally, the gene has been tested for association to�diseases�(Asthma; Breast Neoplasms; Coronary Artery Disease; Osteomalacia) and proposed to participate in a�process�(regulation of transcription, DNA-dependent). Proteins are expected to have molecular�functions�(metal ion binding, protein binding, sequence-specific DNA binding, steroid hormone receptor activity and�2 others) and to�localize�in various compartments (cytoplasm, nucleus). Putativeprotein interactors�have been described (ACTN2, NCOA1, NCOA3, NCOR2, NR1I2, NUCB2, POU1F1, PPARGC1A, PSMC5, RXRA, RXRB, RXRG, SRC).�
Disease
Assays�
(From HuGENavigator)
HIV Infections�
Breast Neoplasms�
Colitis, Ulcerative�
Crohn Disease�
Inflammatory Bowel Diseases�
Neutropenia�
Acquired Immunodeficiency Syndrome�
Colorectal Neoplasms�
Epilepsy�
Drug-Induced Liver Injury�
Kidney Neoplasms�
Carcinoma, Renal Cell�
Cardiovascular Diseases�
Carcinoma�
Multiple Myeloma�
Pregnancy Complications�
Prostatic Neoplasms�
Recurrence�
Respiratory Tract Neoplasms�
Thyroid Neoplasms�
Tobacco Use Disorder�
Translocation, Genetic�
Viremia�
Myocardial Infarction�
Neoplasm Recurrence, Local�
Neoplasms, Second Primary�
Hypertriglyceridemia�
Hypospadias�
Head and Neck Neoplasms�
Hearing Loss�
Osteoporosis, Postmenopausal�
Kidney Failure, Chronic�
Carcinoma, Non-Small-Cell Lung�
Colonic Neoplasms�
Cryptorchidism�
Delayed Graft Function�
Dementia�
Diabetes Mellitus, Type 2�
Cholangitis, Sclerosing�
Cholestasis, Intrahepatic�
Chronic Periodontitis�
Adenocarcinoma�
Anemia�
Asthma�
Barrett Esophagus�
Birth Weight�
Bone Neoplasms�
Leukemia, Myelocytic, Acute�
Leukopenia�
Liver Cirrhosis�
Liver Cirrhosis, Biliary�
Liver Neoplasms�
Lung Neoplasms�
Lymphatic Metastasis�
Lymphoma�
Edema�
Coronary Artery Disease�
Esophageal Neoplasms�
Esophagitis, Peptic�
Fatty Liver�
Interactions
(From STRINGS)
ACTN2, NCOA1, NCOA3, NCOR2, NR1I2, NUCB2, POU1F1, PPARGC1A, PSMC5, RXRA, RXRB, RXRG, SRC
Human Isoforms
(From�Aceview)
The gene contains�12 distinct gt-ag introns. Transcription produces�9 different mRNAs, 7 alternatively spliced variants and 2 unspliced forms. There are 5 probablealternative promotors, 2 non overlapping alternative last exons and 4 validated�alternative polyadenylation sites�(see the�diagram). The mRNAs appear to differ by truncation of the 5' end, truncation of the 3' end, overlapping exons with different boundaries.�Efficacy of translation may be reduced by the presence of a shorter translated product (uORF) initiating at an AUG upstream of the main open reading frame (in variant dAug10).�
Drug Information
(From WikiPedia)
Agonists
5α-Dihydroprogesterone 5β-Dihydroprogesterone 17α-Hydroxypregnenolone 17α-Hydroxyprogesterone Δ4-Androstenedione Δ5-Androstenediol Δ5-Androstenedione AA-861 Allopregnanolone Alpha-Lipoic acid Ambrisentan AMI-193 Amlodipine besylate Antimycotics Artemisinin Aurothioglucose Bile acids Bithionol Bosentan Bumecaine Cafestol Cephaloridine Cephradine Chlorpromazine Ciglitazone Clindamycin Clofenvinfos Chloroxine Clotrimazole Colforsin Corticosterone Cyclophosphamide Cyproterone acetate Demecolcine Dexamethasone DHEA DHEA-S Dibunate sodium Diclazuril Dicloxacillin Dimercaprol Dinaline Docetaxel Docusate calcium Dodecylbenzenesulfonic acid Dronabinol Droxidopa Eburnamonine Ecopipam Enzacamene Epothilone B Erythromycin Famprofazone Febantel Felodipine Fenbendazole Fentanyl Flucloxacillin Fluorometholone Griseofulvin Haloprogin Hetacillin potassium Hyperforin (Hypericum perforatum) Indinavir sulfate Lasalocid sodium Levothyroxine Linolenic acid LOE-908 Loratadine Lovastatin Meclizine Methacycline Methylprednisolone Metyrapone Mevastatin Mifepristone Nafcillin Nicardipine Nicotine Nifedipine Nilvadipine Nisoldipine Norelgestromin Omeprazole Orlistat Oxatomide Paclitaxel Phenobarbital Piperine Plicamycin Prednisolone Pregnanolone Pregnenolone Pregnenolone 16α-carbonitrile Proadifen Progesterone Reserpine Reverse triiodothyronine Rifampicin Rifaximin Rimexolone Riodipine Ritonavir Simvastatin Sirolimus Spironolactone Spiroxatrine SR-12813 Suberoylanilide Sulfisoxazole Suramin Tacrolimus Tenylidone Terconazole Testosterone isocaproate Tetracycline Thiamylal sodium Thiothixene Thonzonium bromide Tianeptine Troglitazone Troleandomycin Tropanyl 3,5-dimethulbenzoate Zafirlukast Zearalanol
Antagonists
Ketoconazole
Expression
(From BioGPS)
References