User:Adam Davis/Sandbox 1
From Proteopedia
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PPARs are ligand-activated transcription factors. The endogenous activators for these receptors are prostaglandins and fatty acids, but synthetic ligands have also been developed for therapeutic use<ref>DOI 10.1016/j.phrs.2004.07.012</ref>. After activation, PPAR forms a heterodimer with the retinoid X receptor, and the complex binds to DNA, either stimulating or repressing transcription of genes involved in glucose or lipid metabolism. | PPARs are ligand-activated transcription factors. The endogenous activators for these receptors are prostaglandins and fatty acids, but synthetic ligands have also been developed for therapeutic use<ref>DOI 10.1016/j.phrs.2004.07.012</ref>. After activation, PPAR forms a heterodimer with the retinoid X receptor, and the complex binds to DNA, either stimulating or repressing transcription of genes involved in glucose or lipid metabolism. | ||
| - | PPARδ is found in many tissues, but is most highly expressed in the gut, kidney, and heart<ref>DOI 10.1210/edrv.20.5.0380</ref>. It is important for fatty acid metabolism, and is known to increase insulin sensitivity<ref>DOI 10.1016/j.pharmthera.2009.12.001</ref>. | + | PPARδ is found in many tissues, but is most highly expressed in the gut, kidney, and heart<ref>DOI 10.1210/edrv.20.5.0380</ref>. It is important for fatty acid metabolism, and is known to increase insulin sensitivity<ref>DOI 10.1016/j.pharmthera.2009.12.001</ref>. Its most well-studied functions include regulation of acyl-CoA synthetase 2 expression and mediation of embryo implantation<ref>DOI 10.1074/jbc.274.50.35881</ref><ref>DOI 10.1101/gad.13.12.1561</ref>. |
== Disease == | == Disease == | ||
Revision as of 12:24, 29 April 2025
PPARδ Bound to GW074
Peroxisome proliferator activated receptors are ligand-activated transcription factors that regulate metabolism of lipids and glucose. They are divided into three families: α, γ, and δ. Activation of PPARδ (which is sometimes also called PPARβ) by endogenous ligands results in increased insulin sensitivity. Synthetic PPARδ agonists hold significant promise for treatment of metabolic and cardiovascular diseases.
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References
- ↑ Batista FA, Trivella DB, Bernardes A, Gratieri J, Oliveira PS, Figueira AC, Webb P, Polikarpov I. Structural Insights into Human Peroxisome Proliferator Activated Receptor Delta (PPAR-Delta) Selective Ligand Binding. PLoS One. 2012;7(5):e33643. Epub 2012 May 11. PMID:22606221 doi:10.1371/journal.pone.0033643
- ↑ doi: https://dx.doi.org/10.1016/j.phrs.2004.07.012
- ↑ doi: https://dx.doi.org/10.1210/edrv.20.5.0380
- ↑ doi: https://dx.doi.org/10.1016/j.pharmthera.2009.12.001
- ↑ doi: https://dx.doi.org/10.1074/jbc.274.50.35881
- ↑ doi: https://dx.doi.org/10.1101/gad.13.12.1561
