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- W2981282186 abstract "The ether analog of lysophosphatidic acid AGP is a high-affinity partial agonist of PPARγ . Binding studies showed that AGP and Rosiglitazone (Rosi) both specifically bind to PPARγ and compete with each other. However, AGP only displaced 40% of bound Rosi. Activation of PPARγ-dependent reporter gene expression showed similar potency, yet AGP-mediated activation was only 40% that of Rosi. A complex between AGP and PPARγ was generated using molecular modeling based on a PPARγ crystal structure. AGP interacting residues were compared with Rosi interacting residues identified within the Rosi-PPARγ co-crystal complex. These comparisons showed that the two ligands occupy partially overlapping positions but make different hydrogen bonding and ion-pairing interactions. Site-specific mutants of PPARγ were prepared to examine their contribution to binding of individual ligands. The H323A and H449A mutants showed reduced binding of Rosi but maintained binding of AGP. In contrast, the R288A mutant showed reduced AGP binding but maintained Rosi binding. Y473A abolished binding and activation by Rosi and AGP. These observations indicate that AGP is a high-affinity ligand of PPARγ but that it binds via interactions distinct from those involved in Rosi binding. This work was supported by grants from USPHS & AHA." @default.
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- W2981282186 date "2006-03-01" @default.
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- W2981282186 title "Differential Recognition of LPA and Rosiglitazone by PPARγ 1" @default.
- W2981282186 doi "https://doi.org/10.1096/fasebj.20.4.a259" @default.
- W2981282186 hasPublicationYear "2006" @default.
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