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Published on: November 17, 2018

Liver X receptors as potential therapeutic targets in atherosclerosis

Yanfei Zhu1, Yousheng Li

  • 1Nanjing University School of Medicine, Research Institute of General Surgery, Jinling Hospital, Nanjing, China.

Clinical and Investigative Medicine. Medecine Clinique Et Experimentale
|October 3, 2009
PubMed
Abstract

Insights

Liver X Receptors (LXRs) show anti-atherosclerosis effects by promoting cholesterol transport and reducing inflammation. New LXR modulators are needed to avoid side effects like increased triglycerides.

Area of Science:

  • Cardiovascular Science
  • Molecular Biology
  • Pharmacology

Background:

  • Atherosclerosis is a major risk factor for cardiovascular disease.
  • Liver X Receptors (LXRs) are implicated in regulating cholesterol homeostasis and inflammation.
  • LXR activation presents a potential therapeutic strategy for atherosclerosis.

Purpose of the Study:

  • To review the physiological roles of LXRs.
  • To examine the link between LXR activity and atherosclerosis.
  • To discuss the therapeutic potential of LXR agonists.

Main Methods:

  • Comprehensive MEDLINE database search using keywords: "liver X receptors", "LXRs", and "atherosclerosis".
  • Manual review of references from identified key articles.

Main Results:

  • LXRs (LXRalpha and LXRbeta) promote reverse cholesterol transport and possess anti-inflammatory properties.
  • LXRalpha regulates hepatic triglyceride synthesis; LXR activation can induce lipogenesis and hypertriglyceridemia.
  • First-generation LXR ligands increase hepatic lipogenesis and plasma triglycerides, necessitating new ligand designs.

Conclusions:

  • LXR beta-selective agonists offer a therapeutic avenue.
  • LXR modulators acting as agonists in macrophages and antagonists in the liver represent a promising approach to treat atherosclerosis and cardiovascular diseases.

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