AC T05687
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ID T05687
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DT 15.10.2003 (created); oke.
DT 23.05.2016 (updated); jtr.
CO Copyright (C), QIAGEN.
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FA CAR
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SY CAR-beta; CAR1; constitutive androstane receptor; constitutively active receptor; MB67 (human); mCAR; mCAR1; NR1I3.
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OS mouse, Mus musculus
OC eukaryota; animalia; metazoa; chordata; vertebrata; tetrapoda; mammalia; eutheria; rodentia; myomorpha; muridae; murinae
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GE G004778 Nr1i3.
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CL C0002; CC (rec); 2.1.2.4.3.
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SF long isoform, homologous to the human CAR and rat CAR, for the short isoform see T02755 [1];
SF binds to DNA as a heterodimer with RXR-alpha, see T05257;
SF activity depends on the conserved C-terminal AF-2 motif [1];
SF CAR AF-2 motif is implicated in ligand-independent transactivation [1];
SF 9th heptad/I box motif is required for heterodimerization [1];
SF phenylalanine at position 171 and isoleucine at 174 are important for interaction with both types of ligands, inverse agonists and agonists [7];
SF constitutive activation function does not depend on positions 171 and 174 [7];
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CP liver, small intestine.
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FF constitutive activator as a heterodimer with RXR-alpha, [1];
FF activates CYP2B gene in response to phenobarbital [3];
FF inverse agonists/inhibiting ligands: steroids androstanol and androstenol [4];
FF treatment with PB and PB-type drugs leads to the nuclear accumulation of CAR in hepatocytes in vivo [5];
FF TCPOBOP, PB-like drug, is a direct agonist ligand [7];
FF functions as a xenobiotic receptor in vivo to mediate response to PB-type drugs [6];
FF activates bilirubin clearance by activation of all 5 enzyme and transporter genes involved and thus provides coordinated response to elevated levels of bilirubin [2];
FF constitutive activity is associated with ligand-independent recruitments of co-activator SRC-1, ligands androstanol and androstenol promote release of SRC-1 form LBD [4];
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IN T09104 FOXO1A; mouse, Mus musculus.
IN T08641 NCOR1-isoform1; mouse, Mus musculus.
IN T01516 Pit-1B; rat, Rattus norvegicus.
IN T08947 SHP; mouse, Mus musculus.
IN T04689 SMRT; human, Homo sapiens.
IN T04632 SRC-1; human, Homo sapiens.
IN T04639 SRC-1; mouse, Mus musculus.
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MX M00966 V$DR3_Q4.
MX M00965 V$DR4_Q2.
MX M07280 V$NR1NR2_Q3.
MX M00964 V$PXR_Q2.
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BS R56213.
BS R37712.
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DR TRANSPATH: MO000037644.
DR TRANSCOMPEL: C00644.
DR UniProtKB: O35627;
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RN [1]; RE0013646.
RX PUBMED: 9295294.
RA Choi H. S., Chung M., Tzameli I., Simha D., Lee Y. K., Seol W., Moore D. D.
RT Differential transactivation by two isoforms of the orphan nuclear hormone receptor CAR
RL J. Biol. Chem. 272:23565-23571 (1997).
RN [2]; RE0023320.
RX PUBMED: 12644704.
RA Huang W., Zhang J., Chua S. S., Qatanani M., Han Y., Granata R., Moore D. D.
RT Induction of bilirubin clearance by the constitutive androstane receptor (CAR).
RL Proc. Natl. Acad. Sci. USA 100:4156-4161 (2003).
RN [3]; RE0023321.
RX PUBMED: 9742082.
RA Honkakoski P., Zelko I., Sueyoshi T., Negishi M.
RT The nuclear orphan receptor CAR-retinoid X receptor heterodimer activates the phenobarbital-responsive enhancer module of the CYP2B gene.
RL Mol. Cell. Biol. 18:5652-5658 (1998).
RN [4]; RE0023325.
RX PUBMED: 9783588.
RA Forman B. M., Tzameli I., Choi H. S., Chen J., Simha D., Seol W., Evans R. M., Moore D. D.
RT Androstane metabolites bind to and deactivate the nuclear receptor CAR-beta.
RL Nature 395:612-615 (1998).
RN [5]; RE0023335.
RX PUBMED: 10454578.
RA Kawamoto T., Sueyoshi T., Zelko I., Moore R., Washburn K., Negishi M.
RT Phenobarbital-responsive nuclear translocation of the receptor CAR in induction of the CYP2B gene.
RL Mol. Cell. Biol. 19:6318-6322 (1999).
RN [6]; RE0023336.
RX PUBMED: 11057673.
RA Wei P., Zhang J., Egan-Hafley M., Liang S., Moore D. D.
RT The nuclear receptor CAR mediates specific xenobiotic induction of drug metabolism.
RL Nature 407:920-923 (2000).
RN [7]; RE0023337.
RX PUBMED: 10757780.
RA Tzameli I., Pissios P., Schuetz E. G., Moore D. D.
RT The xenobiotic compound 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene is an agonist ligand for the nuclear receptor CAR.
RL Mol. Cell. Biol. 20:2951-2958 (2000).
RN [8]; RE0028212.
RX PUBMED: 9372944.
RA Seol W., Chung M., Moore D. D.
RT Novel receptor interaction and repression domains in the orphan receptor SHP.
RL Mol. Cell. Biol. 17:7126-31 (1997).
RN [9]; RE0047375.
RX PUBMED: 11891224.
RA Gonzalez M. M., Carlberg C.
RT Cross-repression, a functional consequence of the physical interaction of non-liganded nuclear receptors and POU domain transcription factors.
RL J. Biol. Chem. 277:18501-18509 (2002).
RN [10]; RE0048304.
RX PUBMED: 15340055.
RA Kodama S., Koike C., Negishi M., Yamamoto Y.
RT Nuclear receptors CAR and PXR cross talk with FOXO1 to regulate genes that encode drug-metabolizing and gluconeogenic enzymes.
RL Mol. Cell. Biol. 24:7931-7940 (2004).
RN [11]; RE0048421.
RX PUBMED: 16219912.
RA Johnson D. R., Li C. W., Chen L. Y., Ghosh J. C., Chen J. D.
RT Regulation and binding of pregnane X receptor by nuclear receptor corepressor silencing mediator of retinoid and thyroid hormone receptors (SMRT).
RL Mol. Pharmacol. 69:99-108 (2006).
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