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Updated: May 25, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
10:51

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists

Published on: November 15, 2013

Natural ligands for nuclear receptors: biology and potential therapeutic applications

Maria Valeria D'Auria1, Valentina Sepe, Angela Zampella

  • 1Dipartimento di Chimica delle Sostanze Naturali, Universita di Napoli "Federico II", VIa D. Montesano 49, 80131 Napoli, Italy.

Current Topics in Medicinal Chemistry
|January 17, 2012
PubMed

Insights

Natural products are increasingly recognized as ligands for nuclear receptors (NRs), impacting reproduction, metabolism, and disease treatment. This review details natural ligands for NR1, NR2, and NR3 subfamilies, highlighting their mechanisms and therapeutic potential.

Area of Science:

  • Endocrinology and pharmacology
  • Molecular biology
  • Natural product chemistry

Background:

  • Nuclear receptors (NRs) regulate critical physiological processes like metabolism and reproduction.
  • NRs are key therapeutic targets for diseases including cancer, diabetes, and liver conditions.
  • Novel NR agonists and antagonists with improved selectivity are sought for drug development.

Purpose of the Study:

  • To review natural products identified as ligands for nuclear receptors.
  • To describe the mechanisms of action and pharmacological profiles of these natural ligands.
  • To emphasize the potential of natural products in NR-targeted drug discovery.

Main Methods:

  • Literature review of studies identifying natural product ligands for NRs.
  • Analysis of reported binding affinities and modes of action.
  • Compilation of pharmacological data for characterized NR-ligand interactions.

Main Results:

  • Numerous natural products have been identified as ligands for NR subfamilies NR1, NR2, and NR3.
  • These natural ligands exhibit significant affinity for their target NRs.
  • Some natural products display unique mechanisms of action, offering novel therapeutic avenues.

Conclusions:

  • Natural products represent a rich source of selective NR modulators.
  • Understanding their mechanisms can guide the development of new NR-targeted therapies.
  • Further exploration of natural products holds promise for treating metabolic and other diseases.

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