Target intelligence / Profile preview

Peroxisome proliferator–activated receptor alpha (PPARα)

Target
PPARα
Molecular classification
Nuclear receptor, Transcription factor, Peroxisome proliferator–activated receptor (PPAR) subfamily, Nuclear hormone receptor superfamily
01

Overview

Peroxisome proliferator–activated receptor alpha (PPARα) is a ligand-activated nuclear transcription factor and a member of the PPAR subfamily within the nuclear hormone receptor superfamily. It plays a master regulatory role in lipid metabolism, glucose homeostasis, inflammation, and vascular biology. Upon activation by endogenous ligands like free fatty acids or synthetic agonists like fibrates, PPARα forms heterodimers with RXR, binds to PPREs in DNA, and regulates the transcription of target genes involved in fatty acid uptake, utilization, and catabolism. It is a key therapeutic target for dyslipidemia and related metabolic disorders.

02

Mechanism of action

Fibrates bind to PPARα, promoting heterodimerization with RXR, binding to PPREs, and modulating gene transcription involved in lipid metabolism and inflammation.

03

Biological functions

Lipid metabolism regulationGlucose homeostasisInflammation suppressionImmune response modulationVascular biology regulationFatty acid transportFatty acid binding/activationMitochondrial/peroxisomal β‐oxidationKetogenesisGluconeogenesisGlycogen synthesis
04

Disease associations

DyslipidemiaCardiovascular diseaseMetabolic syndromeType II diabetes mellitusAtherosclerosis
05

Interacting drugs

Fibrate drugs

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