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Insights into PPARγ from structures with endogenous and covalently bound ligands

Peroxisome proliferator–activated receptor-γ (PPARγ) is a ligand-regulated transcription factor with crucial roles in carbohydrate and lipid metabolism and adipogenesis, but the structural details of the binding and activation by endogenous ligands are not known. Two recent studies reveal how oxidized and nitrated fatty acids uniquely bind and activate PPARγ.

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Figure 1: Helix 12 is a ligand-regulated switch for nuclear receptor transcriptional activity.
Figure 2: Structural details of ligand binding to PPARγ.

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Nettles, K. Insights into PPARγ from structures with endogenous and covalently bound ligands. Nat Struct Mol Biol 15, 893–895 (2008). https://doi.org/10.1038/nsmb0908-893

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