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Related Experiment Videos

Orphan nuclear receptor modulators.

Raju Mohan1, Richard A Heyman

  • 1X-Ceptor Therapeutics, San Diego, CA 92121, USA. Rmohan@x-ceptor.com

Current Topics in Medicinal Chemistry
|December 20, 2003
PubMed
Summary
This summary is machine-generated.

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Orphan nuclear receptors, like LXR and FXR, act as sensors for lipids and bile acids, while PXR and CAR detect foreign compounds. Their modulation offers therapeutic potential for metabolic diseases and cancer.

Area of Science:

  • Endocrinology
  • Molecular Biology
  • Pharmacology

Background:

  • Nuclear hormone receptors are crucial for endocrine signaling and gene regulation.
  • Orphan nuclear receptors, a subset, have incompletely understood functions and targets.
  • Recent research has identified ligands and functions for several orphan nuclear receptors.

Purpose of the Study:

  • To review the discovery of ligands for orphan nuclear receptors (excluding PPARs).
  • To characterize novel signaling pathways and hormone response systems linked to these receptors.
  • To highlight therapeutic opportunities offered by small-molecule modulators.

Main Methods:

  • Literature review of studies on orphan nuclear receptors, their ligands, and functions.
  • Analysis of gene expression patterns and knockout animal studies.

Related Experiment Videos

  • Focus on receptors like LXR, FXR, PXR, CAR, and ERRs.

    • Main Results:

    • LXRs and FXRs regulate lipid and bile acid metabolism.
    • PXRs and CARs act as xenobiotic sensors, influencing drug metabolism and detoxification.
    • PXR induces Cyp3A, impacting hepatoprotection and bile acid metabolism.
    • CAR shows high ligand selectivity, affecting xenobiotic metabolism.

    Conclusions:

    • Orphan nuclear receptors play diverse roles in metabolism, detoxification, and cellular signaling.
    • Ligand identification for ERRs is ongoing, promising further insights.
    • Targeting these receptors with small molecules presents therapeutic avenues for various diseases, including metabolic disorders, inflammation, and cancer.