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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):
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 [2] It was subsequently withdrawn.
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.
Print/export Download as PDF; Printable version; In other projects Wikimedia Commons; Wikidata item; ... Pages in category "Thiazolidinediones"
Print/export Download as PDF; Printable version; In other projects Wikimedia Commons; ... Thiazolidinediones (13 P) Pages in category "Thiazolidines"
It is in the thiazolidinedione (TZD) class and works by improving sensitivity of tissues to insulin. [3] Pioglitazone was patented in 1985, and came into medical use in 1999. [5] It is available as a generic medication. [3] In 2022, it was the 120th most commonly prescribed medication in the United States, with more than 5 million prescriptions.
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