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Retinoid X Receptor agonists as selective modulators of the immune system for the treatment of cancer

Ana S Leal1, Pei-Yu Hung2, Afrin Sultana Chowdhury3

  • 1Department of Pharmacology and Toxicology, Michigan State University, East Lansing, MI, United States of America; Department of Medicine, Indiana University School of Medicine, Indianapolis, IN, United States of America.

Pharmacology & Therapeutics
|November 12, 2023
PubMed

Insights

Retinoid X receptors (RXR) are crucial nuclear receptors that regulate cancer hallmarks. Activating RXR with small molecules can modulate the tumor microenvironment, impacting inflammation and immune responses for cancer therapy.

Area of Science:

  • Nuclear Receptor Signaling
  • Cancer Biology
  • Immunology

Background:

  • Retinoid X receptors (RXR) heterodimerize with other nuclear receptors to form ligand-dependent transcription factors.
  • RXR signaling pathways are critical in regulating various hallmarks of cancer, including inflammation and immune responses.
  • Modulation of the tumor microenvironment by RXR ligands impacts cancer progression and immunity.

Purpose of the Study:

  • To review the mechanisms by which RXR signaling influences inflammation and tumor immunity.
  • To discuss the therapeutic potential of RXR-dependent immune cell modulation in cancer treatment and prevention.
  • To highlight the challenges and opportunities in developing novel RXR agonists for oncology.

Main Methods:

  • Literature review of RXR signaling in cancer.
  • Analysis of small molecule agonists targeting RXR.
  • Discussion of clinical applications and drug discovery programs for RXR modulators.

Main Results:

  • RXR agonists can inhibit cancer cell growth, inflammation, and activate immune cells.
  • Bexarotene is an FDA-approved RXR agonist for cutaneous T cell lymphoma, serving as a benchmark.
  • Numerous novel RXR agonists are under development with promising therapeutic potential.

Conclusions:

  • RXR signaling plays a multifaceted role in regulating cancer inflammation and immunity.
  • Targeting RXR offers a promising strategy for cancer prevention and treatment through immune modulation.
  • Further research and development of RXR agonists are essential to overcome clinical challenges and realize their full therapeutic potential.
Keywords:
RXR agonistsRetinoid X receptorTumor immunityTumor microenvironment

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