What does PPAR-alpha do?

Peroxisome proliferator-activated receptor (PPAR)-alpha is a ligand-activated transcriptional factor that belongs to the family of nuclear receptors. PPAR-alpha regulates the expression of genes involved in fatty acid beta-oxidation and is a major regulator of energy homeostasis.

Where is PPAR-alpha found?

In rodents, highest mRNA expression levels of PPAR-alpha are found in liver and brown adipose tissue, followed by heart and kidney. Lower PPAR-alpha expression levels are found in small and large intestine, skeletal muscle and adrenal gland.

What drug activates PPAR-alpha?

PPAR alpha, agonists

Drug Target Type
Elafibranor Peroxisome proliferator-activated receptor gamma target
Muraglitazar Peroxisome proliferator-activated receptor alpha target
Muraglitazar Peroxisome proliferator-activated receptor gamma target
Muraglitazar Cytochrome P450 1A2 enzyme

What activates PPAR gamma?

The phytocannabinoid cannabidiol (CBD) has been shown to activate PPAR gamma in in vitro and in vivo models. The cannabinoid carboxylic acids THCA, CBDA and CBGA activate PAARy more efficient than their decarboxylated products; however, THCA was the acid found with highest activity.

How do PPAR alpha agonists work?

PPARγ agonists promote adipocyte differentiation, and they promote FFA uptake and storage in subcutaneous adipose rather than visceral adipose tissue. This reduces FFA levels, with associated reductions in insulin resistance.

Is Metformin a PPAR agonist?

Metformin, although not a PPAR agonist, is also commonly used in the treatment of type 2 diabetes.

What is the role of PPAR gamma?

Activation of PPAR-γ causes insulin sensitization and enhances glucose metabolism, whereas activation of PPAR-β/δ enhances fatty acids metabolism. Thus, PPAR family of nuclear receptors plays a major regulatory role in energy homeostasis and metabolic function.

How is PPAR activated?

Physiological function All PPARs heterodimerize with the retinoid X receptor (RXR) and bind to specific regions on the DNA of target genes. These DNA sequences are termed PPREs (peroxisome proliferator hormone response elements). In contrast, PPARα is activated by leukotriene B4.

How does PPAR gamma increase insulin sensitivity?

PPAR-γ agonists decrease circulating triglyceride and free fatty acid levels by repartitioning fatty acids in adipocytes. Increased free fatty acids are associated with hepatic insulin resistance, resulting in the increased gluconeogenesis (47).

What is the role of PPARα in liver metabolism?

Objective Peroxisome proliferator-activated receptor α (PPARα) is a nuclear receptor expressed in tissues with high oxidative activity that plays a central role in metabolism. In this work, we investigated the effect of hepatocyte PPARα on non-alcoholic fatty liver disease (NAFLD).

How does PPARs and nonalcoholic fatty liver disease differ?

PPARs and nonalcoholic fatty liver disease Nonalcoholic fatty liver disease (NAFLD) encompasses a range of liver pathology ranging from simple steatosis to varying degrees of inflammation, hepatocyte injury and fibrosis. Without intervention it can progress to end-stage liver disease and hepatocellular carcinoma. Given its close association …

Which is peroxisome proliferator activated receptor α ( PPARα )?

Peroxisome proliferator-activated receptor α (PPARα) is a ligand-activated transcription factor belonging, together with PPARγ and PPARβ/δ, to the NR1C nuclear receptor subfamily. Many PPARα target genes are involved in fatty acid metabolism in tissues with high oxidative rates such as muscle, heart and liver.

How does the deletion of PPAR alpha affect cisplatin?

PPAR-alpha Deletion Attenuates Cisplatin Nephrotoxicity by Modulating Renal Organic Transporters MATE-1 and OCT-2. PPARalpha/RXRalpha downregulates amino acid catabolism in the liver via interaction with HNF4alpha promoting its proteasomal degradation.