3GWX
MOLECULAR RECOGNITION OF FATTY ACIDS BY PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS
Summary for 3GWX
Entry DOI | 10.2210/pdb3gwx/pdb |
Descriptor | PROTEIN (PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR (PPAR-DELTA)), 5,8,11,14,17-EICOSAPENTAENOIC ACID (3 entities in total) |
Functional Keywords | ppar, fatty acids, transcription, nuclear receptor fold, transcription regulation |
Biological source | Homo sapiens (human) |
Cellular location | Nucleus: Q03181 |
Total number of polymer chains | 2 |
Total formula weight | 62639.02 |
Authors | Xu, H.E.,Lambert, M.H.,Montana, V.G.,Parks, D.J.,Blanchard, S.G.,Brown, P.J.,Sternbach, D.D.,Lehmann, J.M.,Wisely, G.B.,Willson, T.M.,Kliewer, S.A.,Milburn, M.V. (deposition date: 1999-04-26, release date: 2000-04-26, Last modification date: 2023-12-27) |
Primary citation | Xu, H.E.,Lambert, M.H.,Montana, V.G.,Parks, D.J.,Blanchard, S.G.,Brown, P.J.,Sternbach, D.D.,Lehmann, J.M.,Wisely, G.B.,Willson, T.M.,Kliewer, S.A.,Milburn, M.V. Molecular recognition of fatty acids by peroxisome proliferator-activated receptors. Mol.Cell, 3:397-403, 1999 Cited by PubMed Abstract: 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. PubMed: 10198642DOI: 10.1016/S1097-2765(00)80467-0 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.4 Å) |
Structure validation
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