Troglitazone is a TZD which was approved for the treatment of insulin resistance and hyperglycemia in Type II diabetes, under the trade name ResulinTM, but was withdrawn from the market due to hepatotoxicity. Troglitazone is a potent and selective PPAR.gamma. agonist. The EC50 values for transactivation of human and mouse PPAR.gamma. in a cell-based assay are 0.55 and 0.78 uM, respectively. In the same assay system, no activation of PPAR.alpha. and PPAR.delta. was observed at concentrations up to 10 uM. Troglitazone binds to the PPAR.gamma. ligand-binding domain (LBD) but fails to induce interaction of the PPAR.gamma. LBD with the transcriptional coactivators SRC-1, TIF2, AIB1, p300, or TRAP220. Troglitazone also induces cell cycle arrest and apoptosis in several cancer cell lines with an EC50 of 10 uM.
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Troglitazone is a TZD which was approved for the treatment of insulin resistance and hyperglycemia in Type II diabetes, under the trade name ResulinTM, but was withdrawn from the market due to hepatotoxicity. Troglitazone is a potent and selective PPAR.gamma. agonist. The EC50 values for transactivation of human and mouse PPAR.gamma. in a cell-based assay are 0.55 and 0.78 uM, respectively.{10670} In the same assay system, no activation of PPAR.alpha. and PPAR.delta. was observed at concentrations up to 10 uM. Troglitazone binds to the PPAR.gamma. ligand-binding domain (LBD) but fails to induce interaction of the PPAR.gamma. LBD with the transcriptional coactivators SRC-1, TIF2, AIB1, p300, or TRAP220.{8555} Troglitazone also induces cell cycle arrest and apoptosis in several cancer cell lines with an EC50 of 10 uM.{10669}