Target intelligence / Profile preview

Peroxisome proliferator-activated receptor gamma 2 (PPARγ2) (PPARG2)

Target
PPARG2
Molecular classification
Nuclear receptor, Transcription factor, Receptor
01

Overview

Peroxisome proliferator-activated receptor gamma 2 (PPARγ2) is a ligand-activated nuclear transcription factor and a member of the nuclear receptor superfamily. It is primarily expressed in adipose tissue and is distinguished from the PPARγ1 isoform by an additional 30 amino acids at its N-terminus, which confers higher transcriptional activity. PPARγ2 serves as a master regulator of adipogenesis, lipid storage, and glucose metabolism, making it a critical target for treating metabolic disorders. In disease states like type 2 diabetes, its activation improves insulin sensitivity by modulating the expression of genes involved in fatty acid uptake and adipokine secretion. Thiazolidinedione (TZD) drugs, such as pioglitazone and rosiglitazone, act as potent agonists of this receptor to lower blood glucose levels. However, therapeutic use is often limited by side effects such as weight gain and fluid retention, which are largely mediated through its actions in adipose and renal tissues.

Other names
PPAR-gamma 2Nuclear receptor subfamily 1 group C member 3NR1C3Glitazone receptorPPARG
02

Mechanism of action

Ligand-activated transcription factor that heterodimerizes with the Retinoid X Receptor (RXR) to bind to Peroxisome Proliferator Response Elements (PPREs) in the promoter regions of target genes, thereby regulating their expression.

03

Biological functions

AdipogenesisLipid metabolismGlucose homeostasisInsulin sensitivityInflammation regulationCell differentiation
04

Disease associations

Type 2 diabetesObesityMetabolic syndromeInflammationCancerDiabetic nephropathy
05

Safety considerations

Weight gainFluid retention (edema)Congestive heart failure riskBone fracturesBladder cancer risk
06

Interacting drugs

Pioglitazone

5 more in the full profile.

07

Biomarkers

AdiponectinGlycated hemoglobin (HbA1c)Fasting blood glucoseTriglyceridesFree fatty acids

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