The Novel Compounds That Activate Farnesoid X Receptor: the Diversity of Their Effects on Gene Expression
作者: Takuo SuzukiNorimasa TamehiroYoji SatoTetsu KobayashiAkiko Ishii-WatabeYouichi ShinozakiTomoko Nishimaki-MogamiToshihiro HashimotoYoshinori AsakawaKazuhide InoueYasuo OhnoTeruhide YamaguchiToru Kawanishi
作者单位: 1Division of Biological Chemistry and Biologicals, Tokyo 158-8501, Japan
2Division of Biosignaling, Tokyo 158-8501, Japan
3Division of Cellular and Gene Therapy Products, Tokyo 158-8501, Japan
4Division of Pharmacology, National Institute of Health Sciences, Tokyo 158-8501, Japan
5Pharmaceuticals and Medical Device Agency, Tokyo 100-0013, Japan
6Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Tokushima 770-8514, Japan
7Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka 812-8582, Japan
刊名: Journal of Pharmacological Sciences, 2008, Vol.107 (3), pp.285-294
来源数据库: Elsevier Journal
DOI: 10.1254/jphs.08006FP
关键词: Farnesoid X receptor (FXR)Reporter assayGinkgolic acidMarchantinCell-type–specific modulation
原始语种摘要: Abstract(#br)Farnesoid X receptor (FXR) controls the expression of critical genes in bile acid and cholesterol homeostasis. To study FXR and to develop a regulator of cholesterol, some nonsteroidal and steroidal ligands have been found in addition to endogenous ligands for FXR. In this study, we discovered five bile acid derivatives (methyl cholate, methyl deoxycholate, 5 β -cholanic acid, 5 β -cholanic acid-7 α ,12 α -diol, and NIHS700) and two natural products (marchantin A and marchantin E) that activated FXR in the reporter assay. These compounds activated FXR to a high level comparable to the most potent endogenous bile acid, chenodeoxycholic acid, although it was not predicted from their structures; five of them were similar to the lower potency bile acids, and two were structurally...
全文获取路径: Elsevier  (合作)
影响因子:2.15 (2012)

  • expression 表示
  • reporter 报告生成程序
  • although 虽然
  • endogenous 内成的
  • modulation 
  • cholesterol 胆甾醇
  • screened 筛过的
  • addition 添加
  • cholate 胆酸盐或酯
  • specific