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Liver X receptor: a potential target in the treatment of atherosclerosis

Shreya R Savla1, Kedar S Prabhavalkar1, Lokesh K Bhatt1

  • 1Department of Pharmacology, SVKM's Dr. Bhanuben Nanavati College of Pharmacy, Mumbai, India.

Expert Opinion on Therapeutic Targets
|August 25, 2022
PubMed
Abstract

Insights

Liver X receptors (LXRs) regulate cholesterol and inflammation in atherosclerosis. New LXR agonists show therapeutic promise, but LXRα

Area of Science:

  • Cardiovascular Research
  • Molecular Biology
  • Pharmacology

Background:

  • Liver X receptors (LXRs) are key regulators of atherosclerosis, influencing macrophage inflammation and reverse cholesterol transport.
  • Developing novel LXR agonists is crucial for identifying future therapeutic strategies against atherosclerosis.

Purpose of the Study:

  • To review the role of LXRs in atherosclerotic development.
  • To summarize current LXR agonists and explore future research directions in atherosclerosis.

Main Methods:

  • Systematic literature search of PubMed, Scopus, and Google Scholar.
  • Keywords used: atherosclerosis, liver X receptor, LXR agonist.
  • Focus on research from the last 10 years.

Main Results:

  • LXRα regulates cholesterol homeostasis and inflammatory gene expression.
  • LXR agonists face challenges due to LXRα-induced hepatic lipogenesis.
  • Research is exploring cell type-specific knockouts and isoform-specific agonists.

Conclusions:

  • Targeting LXRα and LXRβ, using inverse agonists, or combining agents offers potential therapeutic avenues.
  • Future strategies include targeting ABCA1, M2 macrophages, and LXRα phosphorylation.
Keywords:
ABCA1AtherosclerosisLXR agonistSREBP-1cliver X receptor

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