Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T82702
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| Former ID |
TTDR01273
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| Target Name |
Pregnane X receptor
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| Gene Name |
NR1I2
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| Synonyms |
Orphan nuclear receptor PAR1; SXR; Steroid and xenobiotic receptor; NR1I2
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| Target Type |
Research
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| 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.
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| BioChemical Class |
Zinc-finger
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| Target Validation |
T82702
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| UniProt ID | |||||
| Sequence |
MEVRPKESWNHADFVHCEDTESVPGKPSVNADEEVGGPQICRVCGDKATGYHFNVMTCEG
CKGFFRRAMKRNARLRCPFRKGACEITRKTRRQCQACRLRKCLESGMKKEMIMSDEAVEE RRALIKRKKSERTGTQPLGVQGLTEEQRMMIRELMDAQMKTFDTTFSHFKNFRLPGVLSS GCELPESLQAPSREEAAKWSQVRKDLCSLKVSLQLRGEDGSVWNYKPPADSGGKEIFSLL PHMADMSTYMFKGIISFAKVISYFRDLPIEDQISLLKGAAFELCQLRFNTVFNAETGTWE CGRLSYCLEDTAGGFQQLLLEPMLKFHYMLKKLQLHEEEYVLMQAISLFSPDRPGVLQHR VVDQLQEQFAITLKSYIECNRPQPAHRFLFLKIMAMLTELRSINAQHTQRLLRIQDIHPF ATPLMQELFGITGS |
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| Agonist | 3-keto-lithocholic acid | Drug Info | [1] | ||
| 5beta-cholestane-3alpha,7alpha,12alpha-triol | Drug Info | [2] | |||
| pregnenolone-16alpha-carbonitrile | Drug Info | [3] | |||
| schisandrin A | Drug Info | [4] | |||
| Binder | Hyperforin | Drug Info | [5] | ||
| Inhibitor | WAY-214950 | Drug Info | [6] | ||
| WAY-252623 | Drug Info | [6] | |||
| 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 1 | The 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 2 | Identification 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 3 | An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway. Cell. 1998 Jan 9;92(1):73-82. | ||||
| REF 4 | Traditional 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 5 | Pregnane 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. | ||||
| REF 6 | J 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. | ||||
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