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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
10:51

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists

Published on: November 15, 2013

Expression and activation of the farnesoid X receptor in the vasculature

David Bishop-Bailey1, Desmond T Walsh, Timothy D Warner

  • 1Cardiac, Vascular, and Inflammation Research, William Harvey Research Institute, Barts and the London, Queen Mary University of London, Charterhouse Square, London EC1M 6BQ, United Kingdom. d.bishop-bailey@qmul.ac.uk

Proceedings of the National Academy of Sciences of the United States of America
|March 3, 2004
PubMed

Insights

The farnesoid X receptor (FXR) is found in human vasculature and promotes apoptosis in vascular smooth muscle cells. This nuclear receptor may offer a new therapeutic target for cardiovascular and metabolic diseases.

Area of Science:

  • Molecular Biology
  • Cardiovascular Science
  • Endocrinology

Background:

  • The farnesoid X receptor (FXR), a nuclear hormone receptor, plays roles in cholesterol and bile acid metabolism.
  • FXR ligands are being investigated for cardiovascular disease applications.
  • FXR's presence and function in the vasculature were previously not well-defined.

Purpose of the Study:

  • To investigate the expression and function of FXR in human cardiovascular tissues.
  • To determine the effect of FXR activation on vascular smooth muscle cells.
  • To explore FXR as a potential therapeutic target for vascular and metabolic disorders.

Main Methods:

  • Analysis of FXR expression in a human cardiovascular tissue array.
  • In vitro studies using rat and human vascular smooth muscle cells.
  • Treatment of cells with FXR ligands and assessment of apoptosis and target gene mRNA levels.

Main Results:

  • FXR is expressed in various human tissues, with high levels detected in the vasculature, liver, small intestine, and kidney.
  • FXR is present in vascular smooth muscle cells, and FXR activators induce apoptosis in these cells.
  • FXR activation leads to increased mRNA expression of phospholipid transfer protein and small heterodimer partner.

Conclusions:

  • FXR is a functional protein within the vasculature.
  • FXR activation induces vascular smooth muscle cell apoptosis, suggesting a role in vascular homeostasis.
  • FXR represents a potential therapeutic target for proliferative and dyslipidaemic vascular diseases.

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