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RAR and RXR modulation in cancer and metabolic disease

Lucia Altucci1, Mark D Leibowitz, Kathleen M Ogilvie

  • 1Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico Luigi de Crecchio 7, 80138 Napoli, Italy.

Nature Reviews. Drug Discovery
|October 2, 2007
PubMed

Insights

Retinoic acid receptors (RARs) and retinoid X receptors (RXRs) are key in cell growth. Modulators targeting these receptors show promise for treating cancers and metabolic diseases like diabetes.

Area of Science:

  • Molecular Biology
  • Endocrinology
  • Pharmacology

Background:

  • Retinoic acid receptors (RARs) are transcription factors that form heterodimers with retinoid X receptors (RXRs).
  • RARs and RXRs play crucial roles in regulating cell growth and survival.
  • The therapeutic success of RAR modulation in acute promyelocytic leukaemia (APL) highlights their potential.

Purpose of the Study:

  • To discuss the challenges and opportunities in developing RAR and RXR modulators.
  • To explore therapeutic strategies targeting RARs and RXRs for various diseases.
  • To leverage recent advances in understanding RAR/RXR biology and drug design.

Main Methods:

  • Review of current scientific literature on RAR and RXR biology.
  • Analysis of recent advances in the design of selective receptor modulators.
  • Discussion of therapeutic applications and limitations.

Main Results:

  • Recent advances have improved understanding of RAR and RXR biological roles.
  • Development of selective modulators may overcome limitations of existing drugs.
  • RAR/RXR modulation presents therapeutic opportunities beyond APL.

Conclusions:

  • Targeting RARs and RXRs offers significant potential for treating cancer and metabolic diseases.
  • Further research into selective modulators is warranted to overcome current drug limitations.
  • Understanding RAR/RXR pathways is crucial for developing novel therapeutic strategies.

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