peroxisome proliferator activated receptor binding

Definition

Target type: molecularfunction

Binding to a peroxisome proliferator activated receptor, alpha, beta or gamma. [GOC:jl, PMID:12769781]

Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors that play crucial roles in regulating lipid metabolism, inflammation, and cell differentiation. They are activated by a variety of ligands, including fatty acids, eicosanoids, and synthetic compounds. PPARs function as transcription factors, binding to specific DNA sequences known as peroxisome proliferator response elements (PPREs) in the promoter regions of target genes.

Upon ligand binding, PPARs undergo a conformational change, leading to the recruitment of coactivator proteins. These coactivators facilitate the assembly of a transcription complex at the PPRE, ultimately promoting the transcription of downstream target genes.

PPARs are divided into three subtypes: PPARα, PPARβ/δ, and PPARγ. Each subtype exhibits distinct tissue expression patterns and ligand preferences, contributing to their specific roles in physiological processes.

**PPARα** is primarily expressed in the liver, heart, and skeletal muscle. It plays a key role in fatty acid catabolism, regulating the expression of genes involved in β-oxidation, lipoprotein metabolism, and glucose homeostasis. PPARα activators are used clinically as lipid-lowering agents to treat dyslipidemia and hypertriglyceridemia.

**PPARβ/δ** is ubiquitously expressed and contributes to various metabolic processes, including fatty acid oxidation, glucose utilization, and energy expenditure. It has been implicated in promoting insulin sensitivity and reducing inflammation. PPARβ/δ activators have shown potential as therapeutic agents for metabolic disorders and cancer.

**PPARγ** is predominantly expressed in adipose tissue and plays a critical role in adipogenesis, the differentiation of preadipocytes into mature adipocytes. It also regulates insulin sensitivity and glucose metabolism in peripheral tissues. PPARγ activators are used as antidiabetic drugs to improve insulin sensitivity and reduce hyperglycemia in type 2 diabetes.

The molecular function of peroxisome proliferator-activated receptor binding involves a complex interplay between ligand binding, conformational changes, coactivator recruitment, and transcriptional activation. This process ultimately regulates the expression of genes that control various metabolic, inflammatory, and developmental processes.'
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Proteins (2)

Compounds (20)