Receptor

Peroxisome proliferator-activated receptor

Bioinformatics

Nuclear receptor

Transcription factor

Biology

Gene

Endocrinology

Peroxisome

Peroxisome proliferator-activated receptor alpha

Immunology

Inflammation

Drug

Lipid metabolism

Drug development

Biochemistry

PPAR agonist

Pharmacology

Endocrine Reviews

Peroxisome proliferator–activated receptor α (PPARα) is a nuclear receptor of clinical interest as a drug target in various metabolic disorders. PPARα also exhibits marked anti-inflammatory capacities. The first-generation PPARα agonists, the fibrates, have however been hampered by drug–drug interaction issues, statin drop-in, and ill-designed cardiovascular intervention trials. Notwithstanding, understanding the molecular mechanisms by which PPARα works will enable control of its activities as a drug target for metabolic diseases with an underlying inflammatory component. Given its role in reshaping the immune system, the full potential of this nuclear receptor subtype as a versatile drug target with high plasticity becomes increasingly clear, and a novel generation of agonists may pave the way for novel fields of applications.

Molecular Actions of PPARα in Lipid Metabolism and Inflammation