Pregnane X receptor

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<StructureSection load='1skx' size='450' side='right' caption='Structure of human pregnane X receptor LBD complex with antibiotic rifampicin (PDB entry [[1skx]])' scene='57/571285/Cv/1'>
<StructureSection load='1skx' size='450' side='right' caption='Structure of human pregnane X receptor LBD complex with antibiotic rifampicin (PDB entry [[1skx]])' scene='57/571285/Cv/1'>
== Function ==
== Function ==
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'''Pregnane X receptor''' (PXR) is a [[Nuclear receptor]] which senses the presence of toxic substances and regulates the expression of proteins which are involved in detoxificaton. PXR is activated by a large range of steroids, antibiotics, bile acids and many herbal compounds. Thus it is a generalized sensor of hydrophobic toxins. When activated, PXR binds to the retinoid X receptor (RXR) and the formed heterodimer binds to hormone response elements on the DNA. PXR, similar to other nuclear receptors contains a ligand-binding domain (LBD) and DNA-binding domain (DBD)<ref>PMID:12372848</ref>.
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'''Pregnane X receptor''' (PXR) or '''nuclear receptor subfamily 1 group I member 2''' is a [[Nuclear receptor]] which senses the presence of toxic substances and regulates the expression of proteins which are involved in detoxificaton. PXR is activated by a large range of steroids, antibiotics, bile acids and many herbal compounds. Thus it is a generalized sensor of hydrophobic toxins. When activated, PXR binds to the retinoid X receptor (RXR) and the formed heterodimer binds to hormone response elements on the DNA. PXR, similar to other nuclear receptors contains a ligand-binding domain (LBD) and DNA-binding domain (DBD)<ref>PMID:12372848</ref>.
== Relevance ==
== Relevance ==
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**[[1skx]] – hPXR LBD + antibiotic<br />
**[[1skx]] – hPXR LBD + antibiotic<br />
**[[3r8d]] – hPXR LBD + anti-HIV drug<br />
**[[3r8d]] – hPXR LBD + anti-HIV drug<br />
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**[[1nrl]], [[2o9i]] – hPXR LBD + nuclear receptor coactivator peptide + ligand<br />
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**[[1nrl]], [[2o9i]], [[5a86]] – hPXR LBD + nuclear receptor coactivator peptide + ligand<br />
**[[4j5x]] – hPXR LBD + hRXR LBD + ligand<br />
**[[4j5x]] – hPXR LBD + hRXR LBD + ligand<br />
**[[3hvl]] – hPXR/steroid receptor coactivator + ligand<br />
**[[3hvl]] – hPXR/steroid receptor coactivator + ligand<br />
 +
**[[4ny9]] – hPXR LBD + antagonist<br />
 +
**[[4s0s]], [[4xhd]] – hPXR LBD + adnectin derivative<br />
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**[[4s0t]] – hPXR LBD + adnectin-1 + inhibitor<br />
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**[[4x1f]], [[4x1g]] – hPXR LBD + estrogen derivative<br />
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**[[4xao]] – hPXR LBD + pesticide<br />
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}}
}}
== References ==
== References ==
<references/>
<references/>
[[Category:Topic Page]]
[[Category:Topic Page]]

Revision as of 09:57, 14 September 2017

Structure of human pregnane X receptor LBD complex with antibiotic rifampicin (PDB entry 1skx)

Drag the structure with the mouse to rotate

3D structures of pregnane X receptor

Updated on 14-September-2017

References

  1. Kliewer SA, Goodwin B, Willson TM. The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism. Endocr Rev. 2002 Oct;23(5):687-702. PMID:12372848 doi:http://dx.doi.org/10.1210/er.2001-0038
  2. Koutsounas I, Theocharis S, Patsouris E, Giaginis C. Pregnane X receptor (PXR) at the crossroads of human metabolism and disease. Curr Drug Metab. 2013 Mar;14(3):341-50. PMID:23237007
  3. Chrencik JE, Orans J, Moore LB, Xue Y, Peng L, Collins JL, Wisely GB, Lambert MH, Kliewer SA, Redinbo MR. Structural disorder in the complex of human pregnane X receptor and the macrolide antibiotic rifampicin. Mol Endocrinol. 2005 May;19(5):1125-34. Epub 2005 Feb 10. PMID:15705662 doi:10.1210/me.2004-0346

Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Joel L. Sussman, Alexander Berchansky

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