Target Information

Target General Infomation
Target ID
T82702
Former ID
TTDR01273
Target Name
Pregnane X receptor
Gene Name
NR1I2
Synonyms
Orphan nuclear receptor PAR1; SXR; Steroid and xenobiotic receptor; NR1I2
Target Type
Research
Disease Atherosclerosis [ICD9: 414.0, 440; ICD10: I70]
Function
Orphan receptor; Its natural ligand is probably pregnane. Binds to a response element in the cyp3a4 gene promoter. activates its expression in response to a wide variety of endobiotics and xenobiotics.
BioChemical Class
Zinc-finger
Target Validation
T82702
UniProt ID
O75469
Sequence
MEVRPKESWNHADFVHCEDTESVPGKPSVNADEEVGGPQICRVCGDKATGYHFNVMTCEG
CKGFFRRAMKRNARLRCPFRKGACEITRKTRRQCQACRLRKCLESGMKKEMIMSDEAVEE
RRALIKRKKSERTGTQPLGVQGLTEEQRMMIRELMDAQMKTFDTTFSHFKNFRLPGVLSS
GCELPESLQAPSREEAAKWSQVRKDLCSLKVSLQLRGEDGSVWNYKPPADSGGKEIFSLL
PHMADMSTYMFKGIISFAKVISYFRDLPIEDQISLLKGAAFELCQLRFNTVFNAETGTWE
CGRLSYCLEDTAGGFQQLLLEPMLKFHYMLKKLQLHEEEYVLMQAISLFSPDRPGVLQHR
VVDQLQEQFAITLKSYIECNRPQPAHRFLFLKIMAMLTELRSINAQHTQRLLRIQDIHPF
ATPLMQELFGITGS
Agonist 3-keto-lithocholic acid Drug Info [526000]
5beta-cholestane-3alpha,7alpha,12alpha-triol Drug Info [526500]
pregnenolone-16alpha-carbonitrile Drug Info [534572]
schisandrin A Drug Info [527840]
Binder Hyperforin Drug Info [537021]
Inhibitor WAY-214950 Drug Info [529781]
WAY-252623 Drug Info [529781]
Pathways
WikiPathways Nuclear Receptors in Lipid Metabolism and Toxicity
Nuclear Receptors Meta-Pathway
Pregnane X Receptor pathway
Drug Induction of Bile Acid Pathway
Nuclear Receptors
References
Ref 526000The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3369-74.
Ref 526500Identification of bile acid precursors as endogenous ligands for the nuclear xenobiotic pregnane X receptor. Proc Natl Acad Sci U S A. 2003 Jan 7;100(1):223-8. Epub 2002 Dec 30.
Ref 527840Traditional Chinese medicines Wu Wei Zi (Schisandra chinensis Baill) and Gan Cao (Glycyrrhiza uralensis Fisch) activate pregnane X receptor and increase warfarin clearance in rats. J Pharmacol Exp Ther. 2006 Mar;316(3):1369-77. Epub 2005 Nov 2.
Ref 529781J Med Chem. 2008 Nov 27;51(22):7161-8.Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
Ref 534572An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway. Cell. 1998 Jan 9;92(1):73-82.
Ref 537021Pregnane X receptor (PXR) regulates P-glycoprotein at the blood-brain barrier: functional similarities between pig and human PXR. J Pharmacol Exp Ther. 2009 Apr;329(1):141-9. Epub 2009 Jan 15.

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