Peroxisome proliferator-activated receptor (PPAR) agonists as a potential therapy for inherited metabolic disorders

Biochem Pharmacol. 2023 Mar:209:115433. doi: 10.1016/j.bcp.2023.115433. Epub 2023 Jan 26.

Abstract

Inherited metabolic disorders (IMDs) are genetic disorders that cause a disruption of a specific metabolic pathway leading to biochemical, clinical and pathophysiological sequelae. While the metabolite abnormalities in body fluids and tissues can usually be defined by directed or broad-spectrum metabolomic analysis, the pathophysiology of these changes is often not obvious. Mounting evidence has revealed that secondary mitochondrial dysfunction, mainly oxidative phosphorylation impairment and elevated reactive oxygen species, plays a pivotal role in many disorders. Peroxisomal proliferator-activated receptors (PPARs) consist of a group of nuclear hormone receptors (PPARα, PPARβ/δ, and PPARγ) that regulate multiple cellular functions and processes, including response to oxidative stress, inflammation, lipid metabolism, and mitochondrial bioenergetics and biogenesis. In this context, the activation of PPARs has been shown to stimulate oxidative phosphorylation and reduce reactive species levels. Thus, pharmacological treatment with PPAR activators, such as fibrates, has gained much attention in the last 15 years. This review summarizes preclinical (animal models and patient-derived cells) and clinical data on the effect of PPARs in IMDs.

Keywords: Bezafibrate; Inherited metabolic disorders; Mitochondrial dysfunction; Peroxisome proliferator-activated receptors-PPAR.

Publication types

  • Review

MeSH terms

  • Animals
  • Lipid Metabolism
  • Metabolic Diseases*
  • PPAR alpha
  • PPAR delta*
  • PPAR gamma

Substances

  • PPAR alpha
  • PPAR gamma
  • PPAR delta