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Unraveling the Effects of PPARβ/δ on Insulin Resistance and Cardiovascular Disease

Manuel Vázquez-Carrera1

  • 1Department of Pharmacology and Therapeutic Chemistry, Faculty of Pharmacy, University of Barcelona, Institute of Biomedicine of the University of Barcelona (IBUB), Pediatric Research Institute, Hospital Sant Joan de Déu, Barcelona, Spain; Spanish Biomedical Research Centre in Diabetes and Associated Metabolic Diseases (CIBERDEM)-Instituto de Salud Carlos III, Diagonal 643, 08028 Barcelona, Spain.

Trends in Endocrinology and Metabolism: TEM
|March 24, 2016
PubMed

Insights

Peroxisome proliferator-activated receptor (PPAR) β/δ activators show promise in combating obesity-induced insulin resistance and type 2 diabetes mellitus (T2DM). These compounds may also improve dyslipidemia and cardiovascular disease risk.

Area of Science:

  • Metabolic diseases
  • Pharmacology

Background:

  • Insulin resistance is a precursor to dyslipidemia and type 2 diabetes mellitus (T2DM).
  • Peroxisome proliferator-activated receptor (PPAR) β/δ activators have shown potential in preclinical and clinical studies for metabolic disorders.

Purpose of the Study:

  • To review the mechanistic insights into the antidiabetic effects of PPARβ/δ activators.
  • To examine findings from clinical trials regarding PPARβ/δ activators' efficacy in T2DM and dyslipidemia.

Main Methods:

  • Review of preclinical evidence on PPARβ/δ activators.
  • Analysis of clinical trial data on PPARβ/δ activators.
  • Summary of mechanistic studies on PPARβ/δ actions.

Main Results:

  • PPARβ/δ activators exhibit anti-inflammatory effects and inhibit endoplasmic reticulum (ER) stress.
  • These activators reduce hepatic lipogenesis and improve insulin sensitivity.
  • PPARβ/δ activation mimics pathways stimulated by exercise and may improve atherogenesis.

Conclusions:

  • PPARβ/δ activators offer a potential therapeutic strategy for T2DM and associated dyslipidemia.
  • Understanding PPARβ/δ ligand effects on insulin sensitivity and atherogenesis is crucial for developing new treatments.
  • Targeting PPARβ/δ may help prevent and treat T2DM and cardiovascular disease (CVD).
Keywords:
PPARβ/δinflammationinsulin resistancetype 2 diabetes mellitus

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