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dc.contributor.author김영미-
dc.date.accessioned2018-02-12T05:59:28Z-
dc.date.available2018-02-12T05:59:28Z-
dc.date.issued2015-06-
dc.identifier.citationTOXICOLOGY LETTERS, v. 235, No. 2, Page. 107-115en_US
dc.identifier.issn0378-4274-
dc.identifier.issn1879-3169-
dc.identifier.urihttp://www.sciencedirect.com/science/article/pii/S0378427415001186?via%3Dihub-
dc.identifier.urihttp://hdl.handle.net/20.500.11754/36724-
dc.description.abstractNuclear receptor humanized mice models have been developed to predict regulation of drug metabolizing enzyme by xenobiotics. However, limited information is available concerning xenobiotic-induced regulation of drug metabolizing enzymes in multiple nuclear receptor humanized mice. The present study investigated the hepatic regulation of cytochrome P450s (CYPs) and UDP-glucuronosyl-transferases (UGTs) in the pregnane X receptor (PXR) and the constitutive androstane receptor double humanized mice treated with rifampicin (RIF; 10 mg/kg) for 4 days. RIF increased hepatic microsomal protein and total CYP contents, and CYP reductase activity in the humanized mice, but not in normal mice. Moreover, hepatic induction of Cyp2b10, Cyp2c, and Cyp3a11 were observed only in the RIF-treated humanized mice, suggesting that the humanized mice are sensitive to RIF with respect to the regulation of the hepatic CYP system. Hepatic UGT activities using estradiol, serotonin, and mefenamic acid, but not chenodeoxycholic acid as substrates, increased in the RIF-treated humanized mice, and the glucuronidation activities of estradiol and chenodeoxycholic acid increased in RIF-treated normal mice. These results raise the possibility that a PXR-independent mechanism may be involved in hepatic regulation of UGTs by RIF. (C) 2015 Elsevier Ireland Ltd. All rights reserved.en_US
dc.description.sponsorshipThis study was supported by a grant from the Korea Healthcare Technology R&D Project, Ministry for Health, Welfare, & Family Affairs, Republic of Korea (A101836) and by the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education (2013R1A1A2005981).en_US
dc.language.isoen_USen_US
dc.publisherELSEVIER IRELAND LTDen_US
dc.subjectNuclear receptoren_US
dc.subjectHumanized miceen_US
dc.subjectRifampicinen_US
dc.subjectCytochrome P450en_US
dc.subjectUDP-glucuronosyltransferaseen_US
dc.subjectPREGNANE-X-RECEPTORen_US
dc.subjectCONSTITUTIVE ANDROSTANE RECEPTORen_US
dc.subjectDRUG-DRUG INTERACTIONSen_US
dc.subjectLVER-MICROSOMESen_US
dc.subjectHUMAN HEPATOCYTESen_US
dc.subjectINDUCED TOXICITYen_US
dc.subjectRAT-LIVERen_US
dc.subjectIN-VITROen_US
dc.subjectMETABOLISMen_US
dc.subjectINDUCTIONen_US
dc.titleExpression of hepatic cytochrome P450s and UDP-glucuronosyltransferases in PXR and CAR double humanized mice treated with rifampicinen_US
dc.typeArticleen_US
dc.relation.no2-
dc.relation.volume235-
dc.identifier.doi10.1016/j.toxlet.2015.03.015-
dc.relation.page107-115-
dc.relation.journalTOXICOLOGY LETTERS-
dc.contributor.googleauthorLee, SY-
dc.contributor.googleauthorLee, JY-
dc.contributor.googleauthorKim, YM-
dc.contributor.googleauthorKim, SK-
dc.contributor.googleauthorOh, SJ-
dc.relation.code2015001248-
dc.sector.campusE-
dc.sector.daehakCOLLEGE OF PHARMACY[E]-
dc.sector.departmentDEPARTMENT OF PHARMACY-
dc.identifier.pidymikim12-
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COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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