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Xu, HE, Lambert, MH, Montana, VG, Parks, DJ, Blanchard, SG, Brown, PJ, Sternbach, DD, Lehmann, JM, Wisely, GB, Willson, TM, Kliewer, SA and Milburn, MV (1999) Molecular recognition of fatty acids by peroxisome proliferator-activated receptors. Mol. Cell 3:397-403


The peroxisome proliferator-activated receptors (PPARs) are nuclear receptors for fatty acids (FAs) that regulate glucose and lipid homeostasis. We report the crystal structure of the PPAR delta ligand-binding domain (LBD) bound to either the FA eicosapentaenoic acid (EPA) or the synthetic fibrate GW2433. The carboxylic acids of EPA and GW2433 interact directly with the activation function 2 (AF-2) helix. The hydrophobic tail of EPA adopts two distinct conformations within the large hydrophobic cavity. GW2433 occupies essentially the same space as EPA bound in both conformations. These structures provide molecular insight into the propensity for PPARs to interact with a variety of synthetic and natural compounds, including FAs that vary in both chain length and degree of saturation.




Animals; Binding Sites; Butyric Acids/chemistry; Butyric Acids/metabolism; Crystallization; Crystallography, X-Ray; Eicosapentaenoic Acid/chemistry; Eicosapentaenoic Acid/metabolism; Fatty Acids/chemistry; Fatty Acids/metabolism; Humans; Hydrogen Bonding; Inhibitory Concentration 50; Ligands; Models, Molecular; Molecular Conformation; Phenylurea Compounds/chemistry; Phenylurea Compounds/metabolism; Protein Binding; Protein Conformation; Protein Structure, Secondary; Receptors, Cytoplasmic and Nuclear/chemistry; Receptors, Cytoplasmic and Nuclear/metabolism; Transcription Factors/chemistry; Transcription Factors/metabolism