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Overview
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Background
Rosiglitazone is a potent agonist of peroxisome proliferator-activated receptor γ (PPARγ), a subfamily of the nuclear-receptor superfamily which is predominately expressed in adipose tissue and regulates gene expression responding to ligand binding. Belonging to the thiazolidinedione (TZD) class, rosiglitazone, like other TZD members, binds to PPARγ DNA as heterodimers and activate transcription of various metabolic regulators involved in the differentiation of stem cells into adipocytes and increased expression of genes regulating the metabolism of glucose and lipid. Rosiglitazone is used to treat patients with type II diabetes mellitus for its strong ability to improve insulin sensitization through its effects either on fatty acid uptake and storage in adipose tissue or on adiokines.
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