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Harnessing the benefits of PPARβ/δ agonists

Louise S Mackenzie1, Lisa Lione

  • 1Pharmacology, School of Life and Medical Sciences, University of Hertfordshire, College Lane, Hatfield, AL10 9AB, UK.

Life Sciences
|November 5, 2013
PubMed

Insights

Peroxisome proliferator-activated receptor beta/delta (PPARβ/δ) agonists show therapeutic potential but raise safety concerns. This review explores their dual functions and contrasting study results for future clinical development.

Area of Science:

  • Molecular biology
  • Cellular signaling
  • Pharmacology

Background:

  • Lipid mediators, including PPARβ/δ, play crucial roles in cellular proliferation and inflammation.
  • PPARβ/δ agonists like GW501516 demonstrated therapeutic promise for diabetes.
  • Concerns arose from rodent studies linking GW501516 to tumor development, leading to discontinued research.

Purpose of the Study:

  • To review the dual molecular functions of PPARβ/δ.
  • To connect these functions to diverse in vitro, animal, and human study outcomes.
  • To provide insights into conflicting research results regarding PPARβ/δ agonists.

Main Methods:

  • Literature review of in vitro, animal, and human studies on PPARβ/δ.
  • Analysis of molecular functions and signaling pathways of PPARβ/δ.
  • Comparison of preclinical and clinical findings for PPARβ/δ agonists.

Main Results:

  • PPARβ/δ exhibits complex, dual roles in cellular processes.
  • In vitro studies show varied effects of PPARβ/δ activation.
  • Contrasting outcomes observed between preclinical rodent models and human studies.

Conclusions:

  • Understanding the dual roles of PPARβ/δ is critical for resolving conflicting data.
  • Further research is needed to reconcile diverse findings for safe clinical application.
  • This review aids future development of PPARβ/δ agonists in therapy.
Keywords:
DoseFunctionInduction and transrepressionPPARβ/δPreclinical studies

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