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Updated: Aug 6, 2026

Real Time Monitoring of Intracellular Bile Acid Dynamics Using a Genetically Encoded FRET-based Bile Acid Sensor
Published on: January 4, 2016
Nuclear bile acid receptor FXR as pharmacological target: are we there yet?
Salvatore Modica1, Antonio Moschetta
1Department of Cell Biology and Oncology, Consorzio Mario Negri Sud, Via Nazionale 8A, Santa Maria Imbaro Chieti, CH, Chieti 66030, Italy.
Abstract:
The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that is primarily expressed in the enterohepatic system where it functions as intracellular sensor for bile acids. Ligand dependent FXR activation induces transcriptional responses to coordinately regulate bile acid, cholesterol, triglyceride and glucose metabolism, and to protect the intestinal mucosa from bacterial overgrowth and inflammatory insults. Here we discuss the latest discoveries in FXR-driven metabolic pathways with relevance to pathophysiology and novel therapeutic approaches of several conditions such as hypertriglyceridemia, type 2 diabetes, cholesterol gallstone disease, steato-hepatitis and metabolic syndrome.
Insights
Farnesoid X receptor (FXR) activation regulates metabolism and protects the gut. Discoveries highlight FXR
Area of Science:
- Metabolic pathways and nuclear receptor signaling.
Background:
- The farnesoid X receptor (FXR) is a nuclear receptor primarily in the enterohepatic system.
- FXR acts as an intracellular sensor for bile acids.
- FXR activation regulates bile acid, cholesterol, triglyceride, and glucose metabolism.
Purpose of the Study:
- To discuss recent advancements in FXR-driven metabolic pathways.
- To explore the relevance of these pathways to pathophysiology.
- To review novel therapeutic strategies targeting FXR for metabolic diseases.
Main Methods:
- Literature review of recent discoveries in FXR research.
- Analysis of FXR's role in metabolic regulation.
- Synthesis of information on therapeutic approaches targeting FXR.
Main Results:
- FXR activation influences multiple metabolic processes.
- FXR plays a protective role in the intestinal mucosa.
- FXR-targeted pathways offer therapeutic potential for metabolic disorders.
Conclusions:
- FXR is a key regulator of enterohepatic and metabolic homeostasis.
- Understanding FXR pathways is crucial for treating metabolic diseases.
- Novel FXR-based therapies are emerging for conditions like hypertriglyceridemia, type 2 diabetes, and metabolic syndrome.
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