PXR/RXR Activation
The pregnane X receptor (PXR) is a nuclear receptor that is activated by a spectrum of structurally unrelated endogenous compounds and clinical drugs. Expressed predominantly in the liver and intestine, activated PXR in conjunction with the retinoid X receptor (RXR) plays a central role in drug metabolism by inducing the cytochrome P450 family of enzymes. This includes the induction of CYP3A4, an enzyme responsible for the phase I metabolism of more than 50% of drugs in use today. In addition, PXR/RXR activation induces drug conjugation enzymes as well as the drug efflux pumps. Thus, PXR is an important regulator of drug metabolism and excretion...
Pathway Summary
The pregnane X receptor (PXR) is a nuclear receptor that is activated by a spectrum of structurally unrelated endogenous compounds and clinical drugs. Expressed predominantly in the liver and intestine, activated PXR in conjunction with the retinoid X receptor (RXR) plays a central role in drug metabolism by inducing the cytochrome P450 family of enzymes. This includes the induction of CYP3A4, an enzyme responsible for the phase I metabolism of more than 50% of drugs in use today. In addition, PXR/RXR activation induces drug conjugation enzymes as well as the drug efflux pumps. Thus, PXR is an important regulator of drug metabolism and excretion. PXR/RXR activation can also regulate several endogenous processes like bile acid synthesis, their metabolism and transport, gluconeogenesis, lipid metabolism and cholesterol homeostasis. Thus the PXR/RXR heterodimer plays a fundamental role by regulating the expression of a critical set of protective gene products involved in xenobiotic and endobiotic metabolism.
PXR/RXR Activation Genes list
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ABCB1ATP binding cassette subfamily B member 1 ABCB11ATP binding cassette subfamily B member 11 ABCB9ATP binding cassette subfamily B member 9 ABCC2ATP binding cassette subfamily C member 2 ABCC3ATP binding cassette subfamily C member 3 AKT1AKT serine/threonine kinase 1 AKT2AKT serine/threonine kinase 2 AKT3AKT serine/threonine kinase 3 ALAS15'-aminolevulinate synthase 1 ALDH1A1aldehyde dehydrogenase 1 family member A1 ALDH3A2aldehyde dehydrogenase 3 family member A2 CES2carboxylesterase 2 CES3carboxylesterase 3 CPT1Acarnitine palmitoyltransferase 1A CYP1A2cytochrome P450 family 1 subfamily A member 2 CYP2A6cytochrome P450 family 2 subfamily A member 6 CYP2B6cytochrome P450 family 2 subfamily B member 6 CYP2C19cytochrome P450 family 2 subfamily C member 19 CYP2C8cytochrome P450 family 2 subfamily C member 8 CYP2C9cytochrome P450 family 2 subfamily C member 9 CYP3A4cytochrome P450 family 3 subfamily A member 4 CYP3A5cytochrome P450 family 3 subfamily A member 5 CYP3A7cytochrome P450 family 3 subfamily A member 7 CYP7A1cytochrome P450 family 7 subfamily A member 1 FOXA2forkhead box A2 FOXO1forkhead box O1 G6PC1glucose-6-phosphatase catalytic subunit 1 GSTA1glutathione S-transferase alpha 1 GSTA2glutathione S-transferase alpha 2 GSTM1glutathione S-transferase mu 1 GSTM2glutathione S-transferase mu 2 HMGCS23-hydroxy-3-methylglutaryl-CoA synthase 2 HNF4Ahepatocyte nuclear factor 4 alpha IGFBP1insulin like growth factor binding protein 1 IL6interleukin 6 INSinsulin INSRinsulin receptor NCOA1nuclear receptor coactivator 1 NR0B2nuclear receptor subfamily 0 group B member 2 NR1I2nuclear receptor subfamily 1 group I member 2 NR1I3nuclear receptor subfamily 1 group I member 3 NR3C1nuclear receptor subfamily 3 group C member 1 PAPSS23'-phosphoadenosine 5'-phosphosulfate synthase 2 PCK2phosphoenolpyruvate carboxykinase 2, mitochondrial PPARAperoxisome proliferator activated receptor alpha PPARGC1APPARG coactivator 1 alpha PRKACAprotein kinase cAMP-activated catalytic subunit alpha PRKACBprotein kinase cAMP-activated catalytic subunit beta PRKACGprotein kinase cAMP-activated catalytic subunit gamma PRKAG1protein kinase AMP-activated non-catalytic subunit gamma 1 PRKAG2protein kinase AMP-activated non-catalytic subunit gamma 2 PRKAR1Aprotein kinase cAMP-dependent type I regulatory subunit alpha PRKAR1Bprotein kinase cAMP-dependent type I regulatory subunit beta PRKAR2Aprotein kinase cAMP-dependent type II regulatory subunit alpha PRKAR2Bprotein kinase cAMP-dependent type II regulatory subunit beta RELARELA proto-oncogene, NF-kB subunit RXRAretinoid X receptor alpha SLCO1B3solute carrier organic anion transporter family member 1B3 SULT2A1sulfotransferase family 2A member 1 TNFtumor necrosis factor UGT1A1UDP glucuronosyltransferase family 1 member A1 UGT1A9UDP glucuronosyltransferase family 1 member A9
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