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Target intelligence / Profile preview
Farnesoid X-Activated Receptor (FXR)
- Target
- FXR
- Molecular classification
- Nuclear hormone receptor, Transcription factor
01
Overview
Farnesoid X-Activated Receptor (FXR), also known as Bile Acid Receptor (BAR) or NR1H4, is a ligand-activated nuclear receptor that functions as a transcription factor. Upon activation by bile acids like chenodeoxycholic acid, FXR forms a heterodimer with the retinoid X receptor (RXR) to bind specific DNA response elements and regulate target genes involved in bile acid homeostasis, lipid and glucose metabolism. It is highly expressed in the liver and intestine and plays a crucial role in regulating bile acid synthesis, conjugation, transport, and reabsorption. It is implicated in liver diseases and metabolic disorders and is a drug target.
- Other names
- Farnesoid X receptorBile Acid ReceptorBARNR1H4Nuclear receptor subfamily 1, group H, member 4
02
Mechanism of action
Agonist or antagonist binding modulates gene expression via RXR heterodimerization and DNA binding.
03
Biological functions
Bile acid homeostasisLipid metabolism regulationGlucose metabolism regulationRegulation of gene expressionModulation of microbiotaFluid homeostasis
04
Disease associations
Liver diseaseNonalcoholic steatohepatitis (NASH)Primary biliary cholangitisMetabolic syndromeLiver cancerFibrosis
05
Interacting drugs
Obeticholic acid
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