Target intelligence / Profile preview

Peroxisome Proliferator-Activated Receptor Gamma (PPARγ)

Target
PPARγ
Molecular classification
Nuclear receptor, Transcription factor
01

Overview

Peroxisome proliferator-activated receptor gamma (PPARγ) is a nuclear receptor and ligand-activated transcription factor that regulates genes involved in adipogenesis, lipid metabolism, glucose homeostasis, insulin sensitivity, and inflammation. It plays a central role in energy balance and metabolism and is a therapeutic target for type 2 diabetes.

Other names
PPAR-gammaPPARGNR1C3Nuclear receptor subfamily 1 group C member 3glitazone reverse insulin resistance receptor
02

Mechanism of action

Forms heterodimers with RXRs, binds to PPREs on DNA, recruits coactivators or corepressors to modulate gene transcription involved in energy balance and metabolism. Synthetic agonists like thiazolidinediones improve insulin sensitivity by activating PPARγ-mediated gene programs.

03

Biological functions

Adipocyte differentiationLipid uptakeLipid storageLipid metabolismGlucose homeostasisInsulin sensitivityInflammation controlFluid homeostasisGene regulation
04

Disease associations

Type 2 diabetesCardiovascular diseaseCancerInflammatory disordersMetabolic diseases
05

Safety considerations

Dysregulation or mutation implicated in metabolic diseases, cardiovascular disease, cancer, and inflammatory disorders.Phosphorylation at serine 112 inhibits function and affects insulin sensitivity.
06

Interacting drugs

Rosiglitazone

2 more in the full profile.

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