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Updated: Aug 16, 2026

Real Time Monitoring of Intracellular Bile Acid Dynamics Using a Genetically Encoded FRET-based Bile Acid Sensor
09:21

Real Time Monitoring of Intracellular Bile Acid Dynamics Using a Genetically Encoded FRET-based Bile Acid Sensor

Published on: January 4, 2016

FXR, a therapeutic target for bile acid and lipid disorders

Stefan Westin1, Richard A Heyman, Richard Martin

  • 1Exelixis Inc., 4757 Nexus Centre Drive, San Diego, CA 92121, USA.

Mini Reviews in Medicinal Chemistry
|August 17, 2005
PubMed

Insights

Farnesoid X receptor (FXR), a bile acid sensor, regulates lipid and cholesterol homeostasis. Targeting FXR with drugs offers a promising therapeutic strategy for related metabolic diseases.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Endocrinology

Background:

  • Farnesoid X receptor (FXR) acts as a bile acid sensor in the liver, kidney, and intestine.
  • FXR plays a critical role in maintaining lipid, cholesterol, and bile acid homeostasis.
  • The 'reverse endocrinology' approach aids in understanding orphan nuclear receptors and developing targeted therapies.

Purpose of the Study:

  • To elucidate the physiological role of FXR in metabolic homeostasis.
  • To explore the therapeutic potential of FXR-targeting small molecules.
  • To understand how FXR regulates lipid and bile acid metabolism.

Main Methods:

  • Utilizing the 'reverse endocrinology' strategy to identify FXR ligands.
  • Investigating FXR's regulatory functions in key metabolic tissues.
  • Developing and testing high-affinity synthetic ligands for FXR.

Main Results:

  • FXR's crucial role in cholesterol and bile acid homeostasis was confirmed.
  • Synthetic FXR ligands facilitated the deciphering of its physiological functions.
  • FXR was shown to regulate key transport proteins and biosynthetic enzymes.

Conclusions:

  • FXR is a key regulator of lipid, cholesterol, and bile acid metabolism.
  • Targeting FXR with small-molecule drugs presents a promising therapeutic avenue for metabolic disorders.
  • Understanding FXR's function is vital for developing novel treatments for diseases linked to lipid abnormalities.

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