Pregnane X receptor

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<StructureSection load='' 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='' size='450' side='right' caption='Structure of human pregnane X receptor LBD complex with antibiotic rifampicin (PDB entry [[1skx]])' scene='57/571285/Cv/1'>
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__TOC__
== Function ==
== Function ==
'''Pregnane X receptor''' (PXR) or '''nuclear receptor subfamily 1 group I member 2''' is a [[Nuclear receptors|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>.
'''Pregnane X receptor''' (PXR) or '''nuclear receptor subfamily 1 group I member 2''' is a [[Nuclear receptors|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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PXR regulates the expression of milt-drug protein 1 and other proteins involved in drug metabolism thus affecting the efficacy of chemotherapeutics<ref>PMID:23237007</ref>.
PXR regulates the expression of milt-drug protein 1 and other proteins involved in drug metabolism thus affecting the efficacy of chemotherapeutics<ref>PMID:23237007</ref>.
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== Structural highlights ==
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It plays a crucial role in the body's response to foreign substances, such as drugs, toxins, and endogenous compounds. It is primarily expressed in the liver and intestine, although it can also be found in other tissues, including the kidney and adipose tissue.
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<scene name='57/571285/Cv/3'>PXR ligand-binding pocket is flexible and allows binding to structurally and chemically distinct ligands among them the macrolide antibiotic rifampicin</scene> which is used in testing tuberculosis<ref>PMID:15705662</ref>.
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</StructureSection>
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==3D structures of pregnane X receptor==
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The main function of PXR is to regulate the expression of various drug-metabolizing enzymes and drug transporters. When activated by certain substances, PXR binds to specific regions of DNA called response elements, which are present in the promoter regions of target genes. This binding activates or represses the transcription of these genes, leading to changes in the metabolism and elimination of drugs and other xenobiotics from the body.
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Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
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Activation of PXR can result in increased expression of enzymes such as cytochrome P450s, which are responsible for metabolizing a wide range of drugs and toxins. By inducing these enzymes, PXR helps the body eliminate foreign substances more efficiently. However, it is important to note that PXR activation can also lead to drug-drug interactions and alter the pharmacokinetics and efficacy of certain medications.
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{{#tree:id=OrganizedByTopic|openlevels=0|
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*Pregnane X receptor
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In addition to its role in drug metabolism, PXR is involved in various other biological processes, including lipid and glucose metabolism, inflammation, and the regulation of immune responses.
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**[[1ilg]], [[7ax8]] – hPXR LBD – human<br />
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Overall, the Pregnane X receptor is a critical regulator of xenobiotic metabolism and plays a vital role in maintaining the body's homeostasis in response to various foreign substances.
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**[[3ctb]] – hPXR/steroid receptor coactivator<br />
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**[[4j5w]] – hPXR LBD + hRXR LBD<br />
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*Pregnane X receptor complex
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== Structural highlights ==
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<scene name='57/571285/Cv/3'>PXR ligand-binding pocket is flexible and allows binding to structurally and chemically distinct ligands among them the macrolide antibiotic rifampicin</scene> which is used in testing tuberculosis<ref>PMID:15705662</ref>.
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**[[1ilh]], [[2qnv]] – hPXR LBD + ligand<br />
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==3D structures of pregnane X receptor==
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**[[1m13]] – hPXR LBD + anti-angiogenic<br />
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**[[1skx]] – hPXR LBD + antibiotic<br />
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[[Pregnane X receptor 3D structures]]
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**[[3r8d]] – hPXR LBD + anti-HIV drug<br />
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**[[6hj2]] – hPXR LBD + cancer drug<br />
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**[[4j5x]] – hPXR LBD + hRXR LBD + ligand<br />
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**[[3hvl]], [[1nrl]], [[2o9i]], [[5a86]], [[5x0r]], [[6hty]], [[6nx1]], [[6tfi]], [[6xp9]], [[7chg]] – hPXR/steroid receptor coactivator peptide + ligand<br />
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**[[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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**[[7axi]], [[7axj]], [[7axk]] – hPXR LBD + estrogen derivative + inhibitor<br />
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**[[4xao]] – hPXR LBD + pesticide<br />
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**[[4ny9]], [[6s41]], [[6dup]], [[6p2b]], [[7ax9]], [[7axa]], [[7axb]], [[7axe]], [[7axd]], [[7axe]], [[7axf]], [[7axg]], [[7axh]], [[7axl]], [[7n2a]], [[7rio]], [[7riu]], [[7riv]] – hPXR LBD + inhibitor<br />
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}}
 
== References ==
== References ==
<references/>
<references/>
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</StructureSection>
[[Category:Topic Page]]
[[Category:Topic Page]]

Current revision

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

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Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Joel L. Sussman, Alexander Berchansky

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