Property Summary

NCBI Gene PubMed Count 270
Grant Count 405
R01 Count 263
Funding $48,436,165.79
PubMed Score 1473.48
PubTator Score 825.97

Knowledge Summary

Patent (121,238)

Expression

Synonym

Accession O75469 Q006P5 Q008C8 Q96AC7 Q9UJ22 Q9UJ23 Q9UJ24 Q9UJ25 Q9UJ26 Q9UJ27 Q9UNW4
Symbols BXR
PAR
PRR
PXR
SAR
SXR
ONR1
PAR1
PAR2
PARq

Gene

PDB

1ILG   1ILH   1M13   1NRL   1SKX   2O9I   2QNV   3CTB   3HVL   3R8D   4J5W   4J5X   4NY9   4S0S   4S0T   4X1F   4X1G   4XAO   4XHD   5A86  

 GO Component (1)

MLP Assay (5)

AID Type Active / Inconclusive / Inactive Description
2277 screening 14 / 0 / 0 Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors.
434939 screening 2017 / 0 / 264 Counterscreen for activators of the Aryl Hydrocarbon Receptor (AHR): luminescence-based cell-based high throughput screening assay to identify activators of the Pregnane X Receptor (PXR)
463086 confirmatory 0 / 0 / 126 Luminescence-based counterscreen for activators of the Aryl Hydrocarbon Receptor (AHR): cell-based high throughput dose response screening assay for activators of the Pregnane X Receptor (PXR)
493061 confirmatory 0 / 0 / 33 Late stage counterscreen results for the probe development effort to identify activators of the Aryl Hydrocarbon Receptor (AHR): Luminescence-based cell-based dose response assay for activators of the Pregnane X Receptor (PXR)
504934 other 1 / 0 / 0 Late stage assay provider results from the probe development effort to identify inverse agonists of the liver receptor homolog-1 (LRH-1; NR5A2): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors

Gene RIF (277)

PMID Text
26879815 Reported is the distribution of allelic and genotypic frequencies of IL1A, IL4, NFKB1 and PAR1 variants in Native American, African, and European populations of Brazil and their association with predisposition to cancer.
26549688 SUMOylation at specific sites on PXR protein are involved in enhancement of transcription function of this receptor.
26535635 we found that the PAR1 IVS-14 A/T rs168753 polymorphism was associated with the development of COPD.
26534988 hPXR is regulated through its phosphorylation at threonine-408 by PKC, CHIP/chaperone-dependent stability check, and autophagic degradation pathway.
26504856 PSC is characterized by disease-specific impairment of SULT2A1 expression following PXR activation, a phenomenon which is not noted in PBC, and may account for the impaired hepatoprotection in PSC.
26490116 We found that ARRDC3 is required for ALIX ubiquitination induced by activation of PAR1
26391841 Stimulation of thrombin receptor PAR1 in the model induced cytoplasmic calcium oscillations, calcium uptake by mitochondria, opening of the permeability transition pore and collapse of the mitochondrial membrane potential
26366873 Optical Isomers of Atorvastatin, Rosuvastatin and Fluvastatin Enantiospecifically Activate Pregnane X Receptor PXR and Induce CYP2A6, CYP2B6 and CYP3A4 in Human Hepatocytes.
26355550 Data show that pregnane X receptor/retinoid X receptor PXR/RXR-[alpha], RXR-[beta], or RXR-[gamma] expression was noted in 9 (16.4%), 9 (16.4%), and 10 (18.2%) pancreatic adenocarcinoma cases, respectively.
26340669 decreases of CES and CYP3A4 expression and enzymatic activities induced by Fluoxetine are through decreasing PXR and increasing DEC1 in HepG2 cells
More...

AA Sequence

MEVRPKESWNHADFVHCEDTESVPGKPSVNADEEVGGPQICRVCGDKATGYHFNVMTCEGCKGFFRRAMK      1 - 70
RNARLRCPFRKGACEITRKTRRQCQACRLRKCLESGMKKEMIMSDEAVEERRALIKRKKSERTGTQPLGV     71 - 140
QGLTEEQRMMIRELMDAQMKTFDTTFSHFKNFRLPGVLSSGCELPESLQAPSREEAAKWSQVRKDLCSLK    141 - 210
VSLQLRGEDGSVWNYKPPADSGGKEIFSLLPHMADMSTYMFKGIISFAKVISYFRDLPIEDQISLLKGAA    211 - 280
FELCQLRFNTVFNAETGTWECGRLSYCLEDTAGGFQQLLLEPMLKFHYMLKKLQLHEEEYVLMQAISLFS    281 - 350
PDRPGVLQHRVVDQLQEQFAITLKSYIECNRPQPAHRFLFLKIMAMLTELRSINAQHTQRLLRIQDIHPF    351 - 420
ATPLMQELFGITGS                                                            421 - 434
//

Text Mined References (273)

PMID Year Title
26879815 2016 Distribution of allelic and genotypic frequencies of IL1A, IL4, NFKB1 and PAR1 variants in Native American, African, European and Brazilian populations.
26549688 2016 Transcription regulation of nuclear receptor PXR: Role of SUMO-1 modification and NDSM in receptor function.
26535635 2015 Role of proteinase-activated receptor-1 gene polymorphisms in susceptibility to chronic obstructive pulmonary disease.
26534988 2016 Threonine-408 Regulates the Stability of Human Pregnane X Receptor through Its Phosphorylation and the CHIP/Chaperone-Autophagy Pathway.
26504856 2015 Liver Expression of Sulphotransferase 2A1 Enzyme Is Impaired in Patients with Primary Sclerosing Cholangitis: Lack of the Response to Enhanced Expression of PXR.
26490116 2015 The ?-arrestin ARRDC3 mediates ALIX ubiquitination and G protein-coupled receptor lysosomal sorting.
26391841 2015 Modulation and pre-amplification of PAR1 signaling by ADP acting via the P2Y12 receptor during platelet subpopulation formation.
26366873 2015 Optical Isomers of Atorvastatin, Rosuvastatin and Fluvastatin Enantiospecifically Activate Pregnane X Receptor PXR and Induce CYP2A6, CYP2B6 and CYP3A4 in Human Hepatocytes.
26355550 2015 Pregnane X Receptor Expression in Human Pancreatic Adenocarcinoma: Associations With Clinicopathologic Parameters, Tumor Proliferative Capacity, Patients' Survival, and Retinoid X Receptor Expression.
26340669 2016 Fluoxetine reduces CES1, CES2, and CYP3A4 expression through decreasing PXR and increasing DEC1 in HepG2 cells.
More...