Pioglitazone
From Proteopedia
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| + | <StructureSection load='' size='340' side='right' caption='Pioglitazone, also known as Actos' scene='Pioglitazone/Pioglitazone/1'> | ||
<applet load="" size="480" color="" frame="true" spin="on" Scene ="Pioglitazone/Pioglitazone/1" align="right" caption="Pioglitazone, also known as Actos"/> | <applet load="" size="480" color="" frame="true" spin="on" Scene ="Pioglitazone/Pioglitazone/1" align="right" caption="Pioglitazone, also known as Actos"/> | ||
===Better Known as: Actos=== | ===Better Known as: Actos=== | ||
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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> | ||
| - | + | </StructureSection> | |
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%"> | <table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%"> | ||
Revision as of 14:10, 9 January 2024
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Pharmacokinetics
For Pharmacokinetic Data References, See: References |
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References
- ↑ http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=ACTOS
- ↑ Nolte RT, Wisely GB, Westin S, Cobb JE, Lambert MH, Kurokawa R, Rosenfeld MG, Willson TM, Glass CK, Milburn MV. Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma. Nature. 1998 Sep 10;395(6698):137-43. PMID:9744270 doi:10.1038/25931
