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The retinoid X receptors and their ligands

Marcia I Dawson1, Zebin Xia

  • 1Cancer Center, Sanford-Burn Medical Research Institute, 10901 North Torrey Pines Rd., La Jolla, CA 93207, USA. mdawson@sanfordburnham.org

Biochimica Et Biophysica Acta
|October 25, 2011
PubMed

Insights

This study reviews retinoid X receptor (RXR) subtypes α, β, and γ, detailing their functions, ligands, and structural biology. It highlights how ligand binding affects receptor interactions and explores novel synthetic and natural compounds targeting RXRs.

Area of Science:

  • Molecular Biology
  • Structural Biology
  • Pharmacology

Background:

  • Retinoid X Receptors (RXRs) are crucial nuclear receptors involved in various cellular processes.
  • Understanding RXR structure-function relationships is key to developing targeted therapeutics.

Purpose of the Study:

  • To provide a comprehensive overview of the structural and molecular biology of RXR subtypes α, β, and γ.
  • To discuss the functions, post-transcriptional processing, and diverse ligands of RXRs.
  • To analyze the impact of ligand binding on RXR conformation and interactions.

Main Methods:

  • Literature review of current research on RXR structure and function.
  • Analysis of structural data concerning ligand-binding pocket modifications.
  • Examination of communication pathways between ligand-bound pocket, coactivator surface, and heterodimerization interface.

Main Results:

  • Detailed characterization of RXR subtypes α, β, and γ.
  • Identification of diverse ligands, including natural products, toxins, existing drugs, and novel synthetic compounds.
  • Observation of conformational changes in the ligand-binding pocket induced by various agonists.
  • Trend towards flexible tetraene side chain elements in synthetic RXR ligand design.

Conclusions:

  • RXRs exhibit complex structural dynamics influenced by ligand binding.
  • A growing repertoire of synthetic and natural ligands offers opportunities for RXR-targeted interventions.
  • Further research into RXR modulators holds therapeutic potential.

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