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  • 标题:PPARα Agonists Positively and Negatively Regulate the Expression of Several Nutrient/Drug Transporters in Mouse Small Intestine
  • 本地全文:下载
  • 作者:Toshitake Hirai ; Yuka Fukui ; Kiyoto Motojima
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2007
  • 卷号:30
  • 期号:11
  • 页码:2185-2190
  • DOI:10.1248/bpb.30.2185
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:A systematic analysis to examine the effects of peroxisome proliferator-activated receptor (PPAR)α agonists on the expression levels of all the nutrient/drug plasma-membrane transporters in the mouse small intestine was performed. Transporter mRNAs that were induced or repressed by two independent PPARα-specific agonists were identified by a genome-wide microarray method, and the changes were confirmed by real-time PCR using RNA isolated from the intestines and livers of wild-type and PPARα-null mice. Expression levels of seven nutrient/drug transporters (Abcd3, Octn2/Slc22a5, FATP2/Slc27a2, Slc22a21, Mct13/Slc16a13, Slc23a1 and Bcrp/Abcg2) in the intestine were up-regulated and the expression level of one (Mrp1/Abcc1) was down-regulated by PPARα; although the previously report that the H+/peptide co-transporter 1 (Pept1) is up-regulated by PPARα was not replicated in our study. We propose that the transport processes can be coordinately regulated with intracellular metabolism by nutrient nuclear receptors.
  • 关键词:peroxisome proliferator-activated receptor;transporter;small intestine;microarray;GW7647;drug–drug interaction
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