AC T05671
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ID T05671
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DT 08.09.2003 (created); oke.
DT 15.04.2009 (updated); sva.
CO Copyright (C), QIAGEN.
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FA PXR-isoform1A:RXR-alpha
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OS human, Homo sapiens
OC eukaryota; animalia; metazoa; chordata; vertebrata; tetrapoda; mammalia; eutheria; primates
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CL C0002; CC (rec).
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SF heterodimer, for individual polypeptides see human PXR-isoform1A T04617 and human RXR-alpha T01345;
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FF activator;
FF regulator of xenobiotic response in a complex interplay with CAR:RXR-alpha [3] [5];
FF activates transcription in response to steroids, clotrimazole, rifampicin;
FF provides gene induction by toxic bile acid LCA [6];
FF interacts efficiently and provides gene activation through different types of response elements;
FF may bind to DR3 elements [2] [6];
FF may bind to DR4 elements [3] [4] [5];
FF may bind to ER6/IR6 elements [2] [5];
FF may bind to IR0 elements [6];
FF regulator of liver-specific expression of genes encoding enzymes of xenobiotic metabolism CYP3A, CYP2B, CYP2C [1] [2] [3] [5];
FF activates mdr1 gene whose product is involved in the elimination of many xenobiotics [4];
FF activates genes encoding enzymes of phase II of toxic bile acid elimination [6];
FF PXR:RXR-alpha and CAR:RXR-alpha in several cases regulate common genes through the same DNA elements (regulation by xenobiotics) [3] [5];
FF in other cases PXR:RXR-alpha binds to the same DNA elements with FXR:RXR-alpha (regulation by bile acids) [6];
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MX M00966 V$DR3_Q4.
MX M00965 V$DR4_Q2.
MX M07280 V$NR1NR2_Q3.
MX M03810 V$RXRPXR_Q2.
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BS R18174.
BS R18149.
BS R14174.
BS R14175.
BS R14182.
BS R10090.
BS R10853.
BS R19174.
BS R14176.
BS R14177.
BS R14201.
BS R14202.
BS R14178.
BS R13127.
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DR TRANSPATH: MO000054360.
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RN [1]; RE0016811.
RX PUBMED: 10570062.
RA Goodwin B., Hodgson E., Liddle C.
RT The orphan human pregnane X receptor mediates the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer module.
RL Mol. Pharmacol. 56:1329-1339 (1999).
RN [2]; RE0023228.
RX PUBMED: 9727070.
RA Lehmann J. M., McKee D. D., Watson M. A., Willson T. M., Moore J. T., Kliewer S. A.
RT The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.
RL J. Clin. Invest. 102:1016-1023 (1998).
RN [3]; RE0023235.
RX PUBMED: 11502872.
RA Goodwin B., Moore L. B., Stoltz C. M., McKee D. D., Kliewer S. A.
RT Regulation of the human CYP2B6 gene by the nuclear pregnane X receptor.
RL Mol. Pharmacol. 60:427-431 (2001).
RN [4]; RE0023238.
RX PUBMED: 11297522.
RA Geick A., Eichelbaum M., Burk O.
RT Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin.
RL J. Biol. Chem. 276:14581-14587 (2001).
RN [5]; RE0023246.
RX PUBMED: 11679585.
RA Gerbal-Chaloin S., Daujat M., Pascussi J. M., Pichard-Garcia L., Vilarem M. J., Maurel P.
RT Transcriptional regulation of CYP2C9 gene. Role of glucocorticoid receptor and constitutive androstane receptor.
RL J. Biol. Chem. 277:209-217 (2002).
RN [6]; RE0023250.
RX PUBMED: 12370413.
RA Sonoda J., Xie W., Rosenfeld J. M., Barwick J. L., Guzelian P. S., Evans R. M.
RT Regulation of a xenobiotic sulfonation cascade by nuclear pregnane X receptor (PXR).
RL Proc. Natl. Acad. Sci. USA 99:13801-13806 (2002).
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