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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

Nuclear receptors as drug targets in obesity, dyslipidemia and atherosclerosis

Michael K Hansen1, Thomas M Connolly

  • 1Wyeth Research, Discovery Translational Medicine, 500 Arcola Rd, Collegeville, PA 19426, USA. hansenm@wyeth.com

Current Opinion in Investigational Drugs (London, England : 2000)
|March 4, 2008
PubMed

Insights

Nuclear hormone receptors like PPARs, LXRs, and FXR regulate metabolism. Agonists for these receptors show promise in treating obesity and cardiovascular diseases such as dyslipidemia and atherosclerosis.

Area of Science:

  • Endocrinology and Metabolism
  • Molecular Biology

Background:

  • Nuclear hormone receptors, including peroxisome proliferator-activated receptors (PPARs), liver X receptors (LXRs), and farnesoid X receptor (FXR), are key regulators of metabolic processes.
  • These receptors influence glucose and lipid metabolism, reverse cholesterol transport, and bile acid homeostasis.

Purpose of the Study:

  • To review recent advancements in utilizing PPAR, LXR, and FXR agonists for therapeutic interventions.
  • To discuss the potential of these agonists in managing obesity and cardiovascular conditions like dyslipidemia and atherosclerosis.

Main Methods:

  • Literature review of current research on nuclear hormone receptor agonists.
  • Analysis of preclinical and clinical studies investigating the efficacy of PPAR, LXR, and FXR agonists.

Main Results:

  • PPAR, LXR, and FXR agonists demonstrate significant potential in modulating metabolic pathways relevant to obesity and cardiovascular disease.
  • Evidence suggests these agonists can improve lipid profiles and reduce atherosclerotic burden.

Conclusions:

  • Agonists targeting PPAR, LXR, and FXR represent a promising therapeutic strategy for metabolic and cardiovascular disorders.
  • Further research into currently available drugs and novel therapies is warranted to optimize treatment outcomes.

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