A review of the molecular design and biological activities of RXR agonists

Nathalia Rodrigues de Almeida1, Martin Conda-Sheridan1

  • 1Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, Nebraska.

Insights

Retinoid X receptor (RXR) agonists offer a promising strategy for treating diseases like cancer and diabetes by regulating cell function. This review explores RXR

Area of Science:

  • Molecular Biology
  • Pharmacology
  • Genetics

Background:

  • Nuclear receptors (NRs) regulate crucial cellular functions, including gene transcription.
  • The retinoid X receptor (RXR) is a central NR, interacting with a significant portion of human NRs.
  • Dysregulation of cellular functions mediated by RXR is implicated in diseases such as cancer, diabetes, Alzheimer's, and Parkinson's.

Purpose of the Study:

  • To review the key features of the retinoid X receptor (RXR).
  • To provide a historical perspective on the development of RXR agonists.
  • To discuss diverse RXR-activating compounds, focusing on their structure, activity, and limitations.

Main Methods:

  • Literature review of scientific publications on retinoid X receptor (RXR) agonists.
  • Analysis of molecular structures and biological activities of reported RXR activators.
  • Synthesis of historical data and current research findings.

Main Results:

  • Retinoid X receptors (RXRs) are critical regulators of cellular processes.
  • Various molecular templates have been identified as RXR agonists.
  • Current RXR agonists possess limitations that hinder clinical application.

Conclusions:

  • Targeting retinoid X receptor (RXR) activity is a viable therapeutic strategy for multiple diseases.
  • Further research is needed to overcome limitations of current RXR agonists.
  • Development of novel RXR modulators is essential for clinical translation.

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