Nuclear bile acid receptor FXR as pharmacological target: Are we there yet?

Salvatore Modica, Antonio Moschetta

Research output: Contribution to journalShort surveypeer-review

78 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)5492-5499
Number of pages8
JournalFEBS Letters
Issue number23
StatePublished - Oct 9 2006


  • Cholesterol
  • Farnesoid X receptor
  • Gallstones
  • Hypertriglyceridemia
  • Metabolic syndrome

ASJC Scopus subject areas

  • Biophysics
  • Structural Biology
  • Biochemistry
  • Molecular Biology
  • Genetics
  • Cell Biology


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