title: The role of various peroxisome proliferator-activated receptors and their ligands in clinical practice.
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.
authors.affiliation: Department of Internal Medicine and Therapeutics, Centre of Diabetes and Metabolic Diseases, University of Pavia and Fondazione IRCCS Policlinico S. Matteo, Pavia, Italy.|Laboratory of Molecular Medicine, University of Pavia, Pavia, Italy.|Center for the Study of Endocrine-Metabolic Pathophysiology and Clinical Research, University of Pavia, Pavia, Italy.|Centre for Prevention, Surveillance, Diagnosis and Treatment of Rare Diseases, Fondazione IRCCS Policlinico S. Matteo, Pavia, Italy.
authors.forename: Giuseppe
authors.identifier: http://orcid.org/0000-0003-3573-4760
authors.initials: G
authors.lastname: Derosa
authors.affiliation: Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
authors.forename: Amirhossein
authors.initials: A
authors.lastname: Sahebkar
authors.affiliation: Department of Internal Medicine and Therapeutics, Centre of Diabetes and Metabolic Diseases, University of Pavia and Fondazione IRCCS Policlinico S. Matteo, Pavia, Italy.|PhD School in Experimental Medicine, University of Pavia, Pavia, Italy.
authors.forename: Pamela
authors.initials: P
authors.lastname: Maffioli
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000009:adverse effects / Q000627:therapeutic use*; D000925:Anticoagulants / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D007004:Hypoglycemic Agents / Q000009:adverse effects / Q000627:therapeutic use*; D000960:Hypolipidemic Agents / Q000009:adverse effects / Q000627:therapeutic use*; D008024:Ligands; D047492:Peroxisome Proliferator-Activated Receptors / Q000819:agonists* / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D000893:Anti-Inflammatory Agents; D000925:Anticoagulants; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D008024:Ligands; D047492:Peroxisome Proliferator-Activated Receptors
keywords: cardiovascular disease; diabetes; lipids; metabolism; peroxisome proliferator-activated receptors; therapy