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Published on: March 14, 2020

Liver X receptors as potential therapeutic targets for multiple diseases

Guoqing Cao1, Yu Liang, Xian-Cheng Jiang

  • 1Division of Cardiovascular Discovery, Lilly Research Laboratories, Eli Lilly & Company, Indianapolis, Indiana 46285, USA. Guoqing_Cao@lilly.com

Drug News & Perspectives
|March 3, 2004
PubMed

Insights

Liver X receptors (LXRs) regulate cholesterol, glucose, and inflammation. Selective LXR modulators may offer therapeutic benefits without causing liver fat accumulation, making them promising drug targets.

Area of Science:

  • Molecular biology
  • Metabolic pathways
  • Neuroscience

Background:

  • Liver X receptors alpha (LXRalpha) and beta (LXRbeta) are nuclear receptors that regulate cholesterol homeostasis.
  • Emerging evidence links LXRs to glucose metabolism, inflammation, and Alzheimer's disease pathogenesis.
  • Current LXR agonists can induce hepatic lipogenesis, a potential side effect limiting their therapeutic use.

Purpose of the Study:

  • To review recent advancements in understanding LXR function.
  • To assess the therapeutic potential of LXRs, focusing on selective modulation.
  • To explore strategies for achieving therapeutic benefits while avoiding lipogenesis.

Main Methods:

  • Literature review of studies on LXRalpha and LXRbeta.
  • Analysis of gene regulation by LXR subtypes.
  • Evaluation of LXR agonists and selective modulators in preclinical models.

Main Results:

  • LXRs play a multifaceted role beyond cholesterol, impacting metabolic and inflammatory diseases.
  • Selective LXR modulation strategies are being developed to target specific pathways.
  • Understanding subtype-specific functions is crucial for therapeutic development.

Conclusions:

  • LXRs represent promising therapeutic targets for a range of diseases.
  • Developing subtype-specific agonists or selective modulators is key to maximizing benefits and minimizing side effects like lipogenesis.
  • Further research is warranted to fully elucidate LXR roles and optimize therapeutic strategies.

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