Acetylated deoxycholic (DCA) and cholic (CA) acids are potent ligands of pregnane X (PXR) receptor

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• 作者：Alejandro Carazo^a ; Lucie Hyrsova^a ; Jan Dusek^a ; Hana Chodounska^b ; Alzbeta Horvatova^a ; Karel Berka^c ; Vaclav Bazgier^c ; Hongying Gan-Schreier^d ; Waleé ; Chamulitrat^d ; Eva Kudova^b ; Petr Pavek^a ; ^{petr.pavek@faf.cuni.cz}
• 关键词：BA ; bile acid ; CA ; cholic acid ; CDCA ; chenodeoxycholic acid ; CYP ; cytochrome P450 ; DCA ; deoxycholic acid ; 6-ECDCA ; 6α-ethyl-chenodeoxycholic acid ; obeticholic acid ; FXR ; farnesoid X receptor ; LBD ; ligand binding domain ; LCA ; lithocholic acid ; PXR ; pregnane X receptor ; TR-FRET ; time-resolved fluorescence energy transfer ; VDR ; vitamin D receptor
• 刊名：Toxicology Letters
• 出版年：2017
• 出版时间：4 January 2017
• 年：2017
• 卷：265
• 期：Complete
• 页码：86-96
• 全文大小：2865 K
• 卷排序：265

文摘

Acetylated deoxycholic (DCA) and cholic (CA) acids are potent ligands of PXR. Acetylated DCA and CA enhance PXR target genes expression. Dehydrogenation or acetylation of DCA, CA, lithocholic (LCA) or chenodeoxycholic (CDCA) do not lead to increased affinity to FXR or VDR. Acetylated DCA and CA were not found in bile.