1GWX

MOLECULAR RECOGNITION OF FATTY ACIDS BY PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS

1GWX の概要

• エントリーDOI: 10.2210/pdb1gwx/pdb
• 分子名称: PROTEIN (PPAR-DELTA), 2-(4-{3-[1-[2-(2-CHLORO-6-FLUORO-PHENYL)-ETHYL]-3-(2,3-DICHLORO-PHENYL)-UREIDO]-PROPYL}-PHENOXY)-2-METHYL-PROPIONIC ACID (3 entities in total)
• 機能のキーワード: ppar, fatty acids, transcription, nuclear receptor fold
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Nucleus: Q03181
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 63197.90

構造登録者

Xu, H.E.,Lambert, M.H.,Montana, V.G.,Park, D.J.,Blanchard, S.,Brown, P.,Sternbach, D.,Lehmann, J.,Bruce, G.W.,Willson, T.M.,Kliewer, S.A.,Milburn, M.V. (登録日: 1999-03-17, 公開日: 2000-03-17, 最終更新日: 2023-12-27)

主引用文献

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

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: 10198642
DOI: 10.1016/S1097-2765(00)80467-0

実験手法

X-RAY DIFFRACTION (2.5 Å)