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

Salvatore Modica, Antonio Moschetta

Research output: Contribution to journalArticle

67 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)5492-5499
Number of pages8
JournalFEBS Letters
Volume580
Issue number23
DOIs
StatePublished - Oct 9 2006

Fingerprint

Bile Acids and Salts
Cholesterol
Pharmacology
Hypertriglyceridemia
Gallstones
Intestinal Mucosa
Cytoplasmic and Nuclear Receptors
Medical problems
Metabolic Networks and Pathways
Metabolism
Type 2 Diabetes Mellitus
Transcriptional Activation
Hepatitis
Triglycerides
Chemical activation
Ligands
Glucose
Sensors
Therapeutics
Mucous Membrane

Keywords

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

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

Cite this

Nuclear bile acid receptor FXR as pharmacological target : Are we there yet? / Modica, Salvatore; Moschetta, Antonio.

In: FEBS Letters, Vol. 580, No. 23, 09.10.2006, p. 5492-5499.

Research output: Contribution to journalArticle

Modica, Salvatore ; Moschetta, Antonio. / Nuclear bile acid receptor FXR as pharmacological target : Are we there yet?. In: FEBS Letters. 2006 ; Vol. 580, No. 23. pp. 5492-5499.
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