Target intelligence / Profile preview

Peroxisome Proliferator-Activated Receptor (PPAR)

Target
PPAR
Molecular classification
Nuclear Receptor, Transcription Factor
01

Overview

Peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor proteins that function as ligand-activated transcription factors. They play crucial roles in the regulation of cellular differentiation, development, metabolism (particularly lipid and glucose metabolism), and tumorigenesis in higher organisms. There are three main isoforms: PPARα, PPARγ, and PPARβ/δ, each with distinct tissue distribution, physiological functions, and ligand specificities. Upon activation, PPARs regulate gene transcription by binding to PPREs in the promoter regions of target genes.

Other names
PPARalphaPPARγPPARbeta/delta
02

Mechanism of action

Upon activation by ligands, PPARs heterodimerize with RXR and bind to PPREs in the promoter regions of target genes, modulating gene transcription through recruitment of coactivators or corepressors.

03

Biological functions

Regulation of cellular differentiationDevelopmentLipid metabolismGlucose metabolismGene transcription regulation
04

Disease associations

Diabetes mellitus type 2DyslipidemiaCancerMetabolic Diseases
05

Safety considerations

Alterations in PPAR activity can lead to metabolic diseases.PPARγ agonists may have implications in cancer pathogenesis.
06

Interacting drugs

Thiazolidinediones

2 more in the full profile.

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