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Updated: May 17, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
The significance of the nuclear farnesoid X receptor (FXR) in β cell function
Martina Düfer1, Katrin Hörth, Peter Krippeit-Drews
1Institute of Pharmacy, Department of Pharmacology, University of Tübingen, Tübingen, Germany.
Abstract:
Bile acids (BAs) are important signaling molecules that are involved in the regulation of their own metabolism, lipid metabolism, energy expenditure and glucose homeostasis. The nuclear farnesoid X receptor (FXR) and the G-protein-coupled TGR-5 are the most prominent BA receptors. FXR is highly expressed in liver and activation of liver FXR profoundly affects glucose homeostasis. Strikingly, the effect of FXR activation on glucose metabolism seems to depend on the nutritional status of the organism, i.e., slimness or obesity. Recently, it became evident that FXR is present in pancreatic β cells and that activation of β cell FXR contributes to the regulation of glucose homeostasis. Interestingly, FXR activation increases glucose-induced insulin secretion by non-genomic effects on stimulus-secretion coupling. The first chapter of this review shortly introduces the role of liver FXR in glucose metabolism, the second part focuses on the impact of FXR in lean and obese animals, and the third chapter highlights the significance of FXR in β cells.
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