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.

FEBS Letters
|August 15, 2006
PubMed

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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