Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0Q3RG)
Name
Pregnane X receptor (NR1I2)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Nuclear receptor subfamily 1 group I member 2; Orphan nuclear receptor PAR1; Orphan nuclear receptor PXR; PXR; Pregnane X receptor; SXR; Steroid and xenobiotic receptor
Family Nuclear receptor (NR)  >>  Vitamin D receptor (VDR)
Organism
Homo sapiens (Human)
Gene Name NR1I2 Gene ID
8856
UniProt ID NR1I2_HUMAN (click to find more protein-related data of this DBT)
TTD ID T82702 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MEVRPKESWNHADFVHCEDTESVPGKPSVNADEEVGGPQICRVCGDKATGYHFNVMTCEG
CKGFFRRAMKRNARLRCPFRKGACEITRKTRRQCQACRLRKCLESGMKKEMIMSDEAVEE
RRALIKRKKSERTGTQPLGVQGLTEEQRMMIRELMDAQMKTFDTTFSHFKNFRLPGVLSS
GCELPESLQAPSREEAAKWSQVRKDLCSLKVSLQLRGEDGSVWNYKPPADSGGKEIFSLL
PHMADMSTYMFKGIISFAKVISYFRDLPIEDQISLLKGAAFELCQLRFNTVFNAETGTWE
CGRLSYCLEDTAGGFQQLLLEPMLKFHYMLKKLQLHEEEYVLMQAISLFSPDRPGVLQHR
VVDQLQEQFAITLKSYIECNRPQPAHRFLFLKIMAMLTELRSINAQHTQRLLRIQDIHPF
ATPLMQELFGITGS
Function
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.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Aspartame Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 13 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID NR1I2_HUMAN
          DIG Name: Monothioglycerol Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative; Antioxidant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 5000 nM (estimated based on the structural similarity with CHEMBL1597 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.793103448
                   Tested Species Homo sapiens (Human)
                   UniProt ID NR1I2_HUMAN
          DIG Name: Tert-Butylhydroquinone Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antioxidant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 2000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID NR1I2_HUMAN
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 Identification of clinically used drugs that activate pregnane X receptors. Drug Metab Dispos. 2011 Jan; 39(1):151-9.

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