Investigation on bile acid receptor regulators. Discovery of cholanoic acid derivatives with dual G-protein coupled bile acid receptor 1 (GPBAR1) antagonistic and farnesoid X receptor (FXR) modulatory activity
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- 作者：Valentina Sepea ; Barbara Rengab ; Carmen Festaa ; Claudia Finamorea ; Dario Masulloa ; Adriana Carinob ; Sabrina Ciprianib ; Eleonora Distruttic ; Stefano Fioruccib ; Angela Zampellaa ; angela.zampella@unina.it" class="auth_mail" title="E-mail the corresponding author
- 关键词：BSEP ; bile salt export pump ; CDCA ; chenodeoxycholic acid ; CRE ; cAMP response element ; CREB ; cAMP-response element binding protein ; DMT-MM ; 4-(4 ; 6-dimethoxy-1 ; 3 ; 5-triazin-2-yl)-4-methylmorpholinium chloride ; 6-ECDCA/OCA ; 6-ethylchenodeoxycholic acid/obeticholic acid ; ESI-MS ; electrospray ionization mass spectrometry ; FXR ; farnesoid X receptor ; GPBAR1 ; G protein-coupled bile acid receptor 1 ; HEK293T ; human embryonic kidney 293 cells ; HepG2 ; hepatocellular carcinoma human cell line ; LCA ; lithocholi
- 刊名：Steroids
- 出版年：2016
- 出版时间：January 2016
- 年：2016
- 卷：105
- 期：Complete
- 页码：59-67
- 全文大小：542 K
文摘
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Modification on bile acids resulted in the identification of FXR/GPBAR1 modulators.
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All derivatives were evaluated on FXR and GPBAR1 transactivation.
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Cholanoic acids are the first example of GPBAR1 antagonists.
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Cholanoic acids are novel chemical probes in FXR mediated liver disorders.