2vv3

hPPARgamma Ligand binding domain in complex with 4-oxoDHA

spinqualitylabelsall models 2vv3, resolution 2.85Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2vv3 is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 4R8 Related: 2fvj, 1fm9, 2prg, 1knu, 1rdt, 1i7i, 3prg, 1k74, 1fm6, 1zgy, 1prg, 2f4b, 2vst, 2g0h, 2vsr, 1wm0, 4prg, 2g0g, 1nyx, 2vv0, 2vv1, 2vv2, 2vv4 Resources: FirstGlance, OCA, RCSB, PDBsum Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed The nuclear receptor peroxisome proliferator-activated receptor-gamma (PPARgamma) has important roles in adipogenesis and immune response as well as roles in both lipid and carbohydrate metabolism. Although synthetic agonists for PPARgamma are widely used as insulin sensitizers, the identity of the natural ligand(s) for PPARgamma is still not clear. Suggested natural ligands include 15-deoxy-delta12,14-prostaglandin J2 and oxidized fatty acids such as 9-HODE and 13-HODE. Crystal structures of PPARgamma have revealed the mode of recognition for synthetic compounds. Here we report structures of PPARgamma bound to oxidized fatty acids that are likely to be natural ligands for this receptor. These structures reveal that the receptor can (i) simultaneously bind two fatty acids and (ii) couple covalently with conjugated oxo fatty acids. Thermal stability and gene expression analyses suggest that such covalent ligands are particularly effective activators of PPARgamma and thus may serve as potent and biologically relevant ligands. Structural basis for the activation of PPARgamma by oxidized fatty acids.,Itoh T, Fairall L, Amin K, Inaba Y, Szanto A, Balint BL, Nagy L, Yamamoto K, Schwabe JW Nat Struct Mol Biol. 2008 Sep;15(9):924-31. PMID:19172745 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Peroxisome Proliferator-Activated Receptors

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