Peroxisome Proliferator-Activated Receptor Gamma (PPAR-γ or PPARG) is a type II nuclear receptor that functions as a transcription factor. It is encoded by the PPARG gene in humans and plays a crucial role in regulating gene expression related to glucose and lipid metabolism, adipogenesis, and inflammation .
PPAR-γ is a ligand-activated nuclear receptor that heterodimerizes with the retinoid X receptor (RXR) to regulate the transcription of target genes. The human recombinant form of PPAR-γ, specifically the (1-477 a.a) variant, includes the full-length protein, which is essential for its functional activity .
PPAR-γ is predominantly expressed in adipose tissue, but it is also found in other tissues such as the liver, skeletal muscle, and immune cells. It is a key regulator of adipocyte differentiation and lipid storage. Activation of PPAR-γ by its ligands leads to the transcription of genes involved in fatty acid storage and glucose metabolism, making it a critical player in maintaining energy balance and metabolic homeostasis .
PPAR-γ has been extensively studied for its role in metabolic diseases such as diabetes and obesity. Synthetic agonists of PPAR-γ, such as thiazolidinediones (TZDs), are used as therapeutic agents to improve insulin sensitivity in patients with type 2 diabetes. However, the use of these agonists is limited due to associated side effects, including weight gain and cardiovascular risks .
The recombinant form of PPAR-γ (1-477 a.a) is widely used in research to study its function and regulation. It is also utilized in drug discovery and development to screen for potential PPAR-γ agonists and antagonists. Understanding the molecular mechanisms of PPAR-γ action can lead to the development of more effective and safer therapeutic agents for metabolic disorders .