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Bile acid regulation of gene expression: roles of nuclear hormone receptors

John Y L Chiang1

  • 1Department of Biochemistry and Molecular Pathology, Northeastern Ohio Universities College of Medicine, Rootstown, Ohio 44272, USA. jchiang@neoucom.edu

Endocrine Reviews
|August 31, 2002
PubMed

Insights

Bile acids and oxysterols regulate cholesterol, bile acid, and triglyceride metabolism via nuclear receptors like FXR and LXR. These pathways offer targets for treating cardiovascular and liver diseases.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Endocrinology

Background:

  • Bile acids and oxysterols are crucial signaling molecules regulating cholesterol homeostasis.
  • Nuclear receptors, including FXR and LXR, are key regulators of lipid metabolism.
  • Dysregulation of these pathways is implicated in cardiovascular and liver diseases.

Purpose of the Study:

  • To elucidate the roles of FXR and LXR in coordinating bile acid, cholesterol, and triglyceride metabolism.
  • To highlight the therapeutic potential of targeting nuclear receptors and their regulated genes.

Main Methods:

  • The study reviews the molecular mechanisms by which bile acids and oxysterols interact with FXR and LXR.
  • It examines the downstream effects on gene transcription involved in lipid metabolism and transport.
  • The focus is on understanding the integrated control of metabolic pathways.

Main Results:

  • FXR activation by bile acids inhibits cholesterol 7alpha-hydroxylase and promotes bile acid excretion.
  • LXR activation by oxysterols induces cholesterol 7alpha-hydroxylase, reverse cholesterol transport, and lipogenesis.
  • FXR and LXR coordinately regulate bile acid, cholesterol, and triglyceride metabolism to maintain lipid homeostasis.

Conclusions:

  • FXR and LXR are critical nuclear receptors for maintaining lipid homeostasis.
  • Targeting these nuclear receptors and their regulated genes holds promise for treating metabolic and cardiovascular diseases.
  • Understanding these pathways is essential for developing novel therapeutic strategies.

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