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Screening for liver X receptor modulators: Where are we and for what use?

Julio Buñay1, Allan Fouache1, Amalia Trousson1

  • 1Université Clermont Auvergne, GReD, CNRS, INSERM, and Centre de Recherche en Nutrition Humaine d'Auvergne Clermont-Ferrand, Clermont-Ferrand, France.

British Journal of Pharmacology
|October 20, 2020
PubMed

Insights

Liver X receptors (LXRs) regulate many bodily functions. Modulating LXRs offers potential therapeutic strategies for endocrine, neurological, and inflammatory diseases.

Area of Science:

  • Molecular Endocrinology
  • Nuclear Receptor Superfamily
  • Cholesterol Metabolism

Background:

  • Liver X receptors (LXRs) are nuclear receptors activated by oxidized cholesterol derivatives.
  • LXRs play a crucial role in regulating diverse physiological functions.
  • Genetic modification of LXR expression in mice leads to various endocrine and systemic disorders.

Purpose of the Study:

  • To review the drug discovery landscape for Liver X receptors (LXRs).
  • To explore the therapeutic potential of targeting LXRs for various diseases.
  • To analyze the current status of LXR-modulating drugs in development.

Main Methods:

  • Literature review of LXR research and drug discovery.
  • Analysis of phenotypic consequences of LXR genetic modification in animal models.
  • Survey of available screening tools for LXR modulators.
  • Assessment of the current pipeline for LXR-targeted therapeutics.

Main Results:

  • LXR dysregulation is linked to infertility, diabetes, obesity, neurodegenerative diseases (Alzheimer's, Parkinson's), immune dysfunction, inflammation, and cancer.
  • LXRs are identified as key regulators of lipid metabolism, inflammation, and cellular processes.
  • Numerous studies highlight the potential of LXRs as pharmacological targets.

Conclusions:

  • LXRs represent promising therapeutic targets for a wide range of diseases.
  • Further development of LXR modulators could lead to novel treatments.
  • The review provides an overview of LXR drug discovery tools and developmental progress.
Keywords:
agonistantagonistdrosophiladrug discoveryliver X receptorsnuclear receptor

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