Target intelligence / Profile preview

Peroxisome proliferator–activated receptor delta (PPARδ)

Target
PPARδ
Molecular classification
Nuclear hormone receptor, Transcription factor
01

Overview

Peroxisome proliferator–activated receptor delta (PPARδ) is a nuclear hormone receptor that functions as a ligand-dependent transcription factor. It regulates genes involved in lipid and glucose metabolism, cellular differentiation, inflammation, and other processes. Activated by fatty acids and eicosanoids, it forms heterodimers with RXRs to bind PPREs and modulate gene expression. PPARδ plays roles in metabolic regulation, cardiovascular function, and potentially cancer, with studies showing conflicting evidence for its role in tumor progression.

Other names
PPAR-deltaPPARβPPAR-betaNUC1Nuclear hormone receptor 1PPARD
02

Mechanism of action

Upon ligand binding, PPARδ forms heterodimers with retinoid X receptors (RXRs). This complex binds to specific DNA sequences called peroxisome-proliferator response elements (PPREs) within target gene promoters to regulate transcription.

03

Biological functions

Lipid metabolismGlucose metabolismCellular differentiationInflammation modulationMyelination of the central nervous systemDirectional sensingPolarizationMigration in keratinocytesRegulation of gene transcription
04

Disease associations

Metabolic disordersCardiovascular diseaseCancer
05

Safety considerations

Potential for promoting tumor angiogenesisMixed studies regarding role in cancer progression
06

Interacting drugs

GW501516

1 more in the full profile.

07

Biomarkers

PDK4ANGPTL4PLIN2CD36

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