The role of various peroxisome proliferator-activated receptors and their ligands in clinical practice

Giuseppe Derosa, Amirhossein Sahebkar, Pamela Maffioli

Research output: Contribution to journalReview article

Abstract

Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors involved in several physiological processes including modulation of cellular differentiation, development, metabolism of carbohydrates, lipids, proteins, and tumorigenesis. The aim of this review is to examine how different PPAR ligands act, and discuss their use in clinical practice. PPAR ligands have a lot of effects and applications in clinical practice. Some PPAR ligands such as fibrates (PPAR-α ligands) are currently used for the treatment of dyslipidemia, while pioglitazone and rosiglitazone (PPAR-γ ligands) are anti-diabetic and insulin-sensitizing agents. Regarding new generation drugs, acting on both α/γ, β/δ, or α/δ receptors simultaneously, preliminary data on PPAR-α/γ dual agonists revealed a positive effect on lipid profile, blood pressure, atherosclerosis, inflammation, and anti-coagulant effects, while the overexpression of PPAR-β/δ seems to prevent obesity and to decrease lipid storage in cardiac cells. Finally, PPAR-α/δ dual agonist induces resolution of nonalcoholic steatohepatitis without fibrosis worsening.

Original languageEnglish
Pages (from-to)153-161
Number of pages9
JournalJournal of Cellular Physiology
Volume233
Issue number1
DOIs
Publication statusPublished - Jan 1 2018

Keywords

  • cardiovascular disease
  • diabetes
  • lipids
  • metabolism
  • peroxisome proliferator-activated receptors
  • therapy

ASJC Scopus subject areas

  • Physiology
  • Clinical Biochemistry
  • Cell Biology

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