1998
DOI: 10.1074/jbc.273.47.31108
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Crystal Structure of the Ligand Binding Domain of the Human Nuclear Receptor PPARγ

Abstract: The peroxisome proliferator-activated receptors (PPAR) are members of the nuclear receptor supergene family and are considered as key sensors of both lipid and glucose homeostasis. The role of the PPAR␥ isoform in glucose metabolism is illustrated by the fact that antidiabetic thiazolidinediones have been shown to be bona fide PPAR␥ ligands. Here we report the crystal structure of apo-PPAR␥ ligand binding domain (LBD) determined to 2.9-Å resolution. Although the structure of apo-PPAR␥-LBD retains the overall f… Show more

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Cited by 247 publications
(159 citation statements)
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“…Resolutions of the complexes were 2.8, 3.15, and 2.9 Å, respectively ( Table I). The overall fold of the PPAR␥-LBD shows only minor differences as compared with the previously determined apoPPAR␥ structure (26). The major differences are in the region connecting helix 2Ј and helix 3, a region with high mobility.…”
Section: Identification Of a Novel Class Of Ppar Ligands-mentioning
confidence: 70%
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“…Resolutions of the complexes were 2.8, 3.15, and 2.9 Å, respectively ( Table I). The overall fold of the PPAR␥-LBD shows only minor differences as compared with the previously determined apoPPAR␥ structure (26). The major differences are in the region connecting helix 2Ј and helix 3, a region with high mobility.…”
Section: Identification Of a Novel Class Of Ppar Ligands-mentioning
confidence: 70%
“…Furthermore, the 2-BABAs are situated at the entrance of the active site and do not interact directly with helix 12. There are three unrelated crystallographic apo structures of PPAR␥ (21,26), of which two closely resemble the agonistic structures in terms of helix 12 position and interactions, thus giving no hints of conformational changes related to ligand activation. In the third structure helix 12 adopts a different conformation, slightly protruding away from the LBD, and could therefore more easily be interpreted as an inactive state.…”
Section: Discussionmentioning
confidence: 99%
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