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Thiazolidinedione ligand dependent transactivation is responsible for the majority of anti-diabetic effects. The activated PPAR/RXR heterodimer binds to peroxisome proliferator hormone response elements upstream of target genes in complex with a number of coactivators such as nuclear receptor coactivator 1 and CREB binding protein, this causes upregulation of genes (for a full list see PPARγ):
Thiazolidines functionalized with carbonyls at the 2 and 4 positions, the thiazolidinediones, are drugs used in the treatment of diabetes mellitus type 2. Rhodanine is a related bioactive species, featuring one carbonyl and one thiocarbonyl. Many thiazolidines are prepared from cysteine and related aminothiols.
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. Known inhibitors include the experimental agent GW-9662.
The anti diabetic thiazolidinediones activate PPARγ. [citation needed] The synthetic chemical perfluorooctanoic acid activates PPARα while perfluorononanoic acid activates both PPARα and PPARγ. [citation needed] Berberine inactivates PPARγ. Huang C, Zhang Y, Gong Z, Sheng X, Li Z, Zhang W, Qin Y (2006).
Thiazolidinediones bind to PPARγ. PPARs are expressed in fat cells, cells of the liver, muscle, heart, and inner wall (endothelium) and smooth muscle of blood vessels. PPARγ is expressed mainly in fat tissue, where it regulates genes involved in fat cell (adipocyte) differentiation, fatty acid uptake and storage, and glucose uptake.
Troglitazone is an antidiabetic and anti-inflammatory drug, and a member of the drug class of the thiazolidinediones. It was prescribed for people with diabetes mellitus type 2. [1] It was patented in 1983 and approved for medical use in 1997. [2] It was subsequently withdrawn.
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Thiazolidinediones (Tzd) – pioglitazone, Actos generic; Alpha-glucosidase inhibitors – Acarbose; Meglitinides – nateglinide; Combination of sulfonylureas plus metformin – known by generic names of the two drugs; No generics are available for dipeptidyl peptidase-4 inhibitors (Onglyza), the glifozins, the incretins and various combinations.