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dc.contributor.author전대원-
dc.date.accessioned2017-09-08T01:57:20Z-
dc.date.available2017-09-08T01:57:20Z-
dc.date.issued2015-11-
dc.identifier.citationJOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, v. 355, NO 3, Page. 362-369en_US
dc.identifier.issn0022-3565-
dc.identifier.issn1521-0103-
dc.identifier.urihttp://jpet.aspetjournals.org/content/355/3/362-
dc.identifier.urihttp://hdl.handle.net/20.500.11754/28978-
dc.description.abstractLiver X receptor (LXR) is a member of the nuclear receptor superfamily, and it regulates various biologic processes, including de novo lipogenesis, cholesterol metabolism, and inflammation. Selective inhibition of LXR may aid the treatment of nonalcoholic fatty liver diseases. In the present study, we evaluated the effects of three cinnamamide derivatives on ligand-induced LXR alpha activation and explored whether these derivatives could attenuate steatosis in mice. N-(4-trifluoromethylphenyl) 3,4-dimethoxycinnamamide (TFCA) decreased the luciferase activity in LXRE-tk-Luc-transfected cells and also suppressed ligand-induced lipid accumulation and expression of the lipogenic genes in murine hepatocytes. Furthermore, it significantly attenuated hepatic neutral lipid accumulation in a ligand-induced fatty liver mouse system. Modeling study indicated that TFCA inhibited activation of the LXR alpha ligand-binding domain by hydrogen bonding to Arg305 in the H5 region of that domain. It regulated the transcriptional control exerted by LXR alpha by influencing coregulator exchange; this process involves dissociation of the thyroid hormone receptor-associated proteins (TRAP)/DRIP coactivator and recruitment of the nuclear receptor corepressor. These results show that TFCA has the potential to attenuate ligand-induced lipogenesis and fatty liver by selectively inhibiting LXR alpha in the liver.en_US
dc.description.sponsorshipThis work was supported by grants of the Korea Healthcare Technology R&D Project, Ministry of Health & Welfare, Republic of Korea (A121185).en_US
dc.language.isoenen_US
dc.publisherAMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICSen_US
dc.subjectELEMENT-BINDING PROTEIN-1Cen_US
dc.subjectCINNAMIC ACID-DERIVATIVESen_US
dc.subjectLXR-ALPHAen_US
dc.subjectNUCLEAR RECEPTORSen_US
dc.subjectGENE-EXPRESSIONen_US
dc.subjectINSULIN-RESISTANCEen_US
dc.subjectSREBP-1Cen_US
dc.subjectAGONISTen_US
dc.subjectINFLAMMATIONen_US
dc.subjectSTIMULATIONen_US
dc.titleCinnamamides, Novel Liver X Receptor Antagonists that Inhibit Ligand-Induced Lipogenesis and Fatty Liveren_US
dc.typeArticleen_US
dc.relation.no3-
dc.relation.volume355-
dc.identifier.doi10.1124/jpet.115.226738-
dc.relation.page362-369-
dc.relation.journalJOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS-
dc.contributor.googleauthorSim, Woo-Cheol-
dc.contributor.googleauthorKim, Dong Gwang-
dc.contributor.googleauthorLee, Kyeong Jin-
dc.contributor.googleauthorChoi, You-Jin-
dc.contributor.googleauthorChoi, Yeon Jae-
dc.contributor.googleauthorShin, Kye Jung-
dc.contributor.googleauthorJun, Dae Won-
dc.contributor.googleauthorPark, So-Jung-
dc.contributor.googleauthorPark, Hyun-Ju-
dc.contributor.googleauthorKim, Jiwon-
dc.relation.code2015001010-
dc.sector.campusS-
dc.sector.daehakCOLLEGE OF MEDICINE[S]-
dc.sector.departmentDEPARTMENT OF MEDICINE-
dc.identifier.pidnoshin-
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COLLEGE OF MEDICINE[S](의과대학) > MEDICINE(의학과) > Articles
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