Thiazolidinediones (TZDs)1 are a new class of hypoglycemic agents that improve peripheral insulin resistance (1). TZDs bind and activate peroxisome proliferator-activated receptor γ (PPARγ), a key transcription factor involved in glucose and lipid metabolism, and adipose differentiation (2, 3, 4, 5).
Q. Which antidiabetics is a highly selective and potent agonist for the peroxisome proliferator-activated receptor gamma?
Rosiglitazone is an antidiabetic agent (thiazolidinedione derivative) that improves glycemic control by enhancing insulin sensitivity. The drug is a potent, highly selective agonist for the peroxisome proliferator-activated receptor-gamma (PPAR-gamma).
Q. What is peroxisome proliferator-activated receptor agonist?
Peroxisome proliferator-activated receptor (PPAR) agonists have emerged as promising repurposed drugs due to their anti-inflammatory activities. PPARs are Type II nuclear receptors, which function in complexes as ligand-activated transcription factors and are best known for their roles in development and metabolism.
Q. What activates peroxisome proliferator?
PPARs are activated by endogenous ligands that are derived from the metabolism of fatty acids and other compounds that are found in the diet, which is consistent with the fact that PPARs regulate the expression of many genes involved in glucose and lipid metabolism1.
Q. Which drug is PPAR gamma activator?
Thiazolidinediones (TZDs) agonists for peroxisome proliferators-activated receptor (PPAR) γ are currently used therapeutically. Troglitazone, the first agent of this class to be approved, was effective in controlling glycemia but was removed from the market because of serious liver toxicity.
Q. Are there any peroxisome proliferator activated receptor ( PPAR ) agonists?
Thiazolidinediones (TZDs) agonists for peroxisome proliferators-activated receptor (PPAR) γ are currently used therapeutically. Troglitazone, the first agent of this class to be approved, was effective in controlling glycemia but was removed from the market because of serious liver toxicity.
Q. Which is an agonist of the PPAR gamma group?
PPAR-gamma agonists PPARγ (gamma) is the main target of the drug class of thiazolidinediones (TZDs), used in diabetes mellitus and other diseases that feature insulin resistance. It is also mildly activated by certain NSAIDs (such as ibuprofen) and indoles, as well as from a number of natural compounds.
Q. How are PPAR agonists used to treat metabolic syndrome?
PPAR-alpha and -gamma pathways. PPAR agonists are drugs which act upon the peroxisome proliferator-activated receptor. They are used for the treatment of symptoms of the metabolic syndrome, mainly for lowering triglycerides and blood sugar.
Q. Are there any PPARγ agonists for type 2 diabetes?
Pioglitazone and Rosiglitazone are PPARγ agonists currently licensed for the management of hyperglycemia in Type 2 diabetes mellitus (T2DM). TZDs induced glycemic improvement is accompanied by a significant reduction in fasting insulin.
