Pioglitazone: Difference between revisions
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===Mechanism of Action=== | ===Mechanism of Action=== | ||
Pioglitazone is a selective agonist for Peroxisome Proliferator-Activated Receptor Gamma ([[PPAR]]). When PPAR is not bound by ligand, it forms a complex with various co-repressors which possess histone deacetylation activity, maintaining tight chromatin structure and preventing gene transcription. This complex is released upon ligand binding (typical ligands are lipids), allowing various co-activators and co-activator-associated proteins to be recruited. Pioglitazone functions by by binding to the active site of PPARγ, causing the release of co-repressors and activation of the receptor. Activation of PPAR results in transcription of [[Molecular Playground/Insulin|insulin]] responsive genes involved in the control of glucose production, transport and utilization. This explains why the glitazones are referred to as "insulin sensitizers." <ref>PMID:9744270</ref> | Pioglitazone is a selective agonist for Peroxisome Proliferator-Activated Receptor Gamma ([[PPAR]]). When PPAR is not bound by ligand, it forms a complex with various co-repressors which possess histone deacetylation activity, maintaining tight chromatin structure and preventing gene transcription. This complex is released upon ligand binding (typical ligands are lipids), allowing various co-activators and co-activator-associated proteins to be recruited. Pioglitazone functions by by binding to the active site of PPARγ, causing the release of co-repressors and activation of the receptor. Activation of PPAR results in transcription of [[Molecular Playground/Insulin|insulin]] responsive genes involved in the control of glucose production, transport and utilization. This explains why the glitazones are referred to as "insulin sensitizers." <ref>PMID:9744270</ref> | ||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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