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dc.contributor.authorLi, Yong
dc.contributor.author李勇
dc.contributor.authorJin, Lihua
dc.contributor.author金利华
dc.contributor.authorLin, Shengchen
dc.contributor.authorRong, Hui
dc.contributor.authorZheng, Songyang
dc.contributor.authorJin, Shikan
dc.contributor.authorWang, Rui
dc.date.accessioned2012-03-29T07:49:34Z
dc.date.available2012-03-29T07:49:34Z
dc.date.issued2011-07-20
dc.identifier.citationJ Biol Chem. 2011 Sep 9;286(36):31473-9.zh_CN
dc.identifier.issn0021-9258
dc.identifier.urihttp://dx.doi.org/doi:10.1074/jbc.M111.266023
dc.identifier.uriWOS:000294487500042
dc.identifier.urihttps://dspace.xmu.edu.cn/handle/2288/11925
dc.description.abstractIloprost is a prostacyclin analog that has been used to treat many vascular conditions. Peroxisome proliferator-activated receptors (PPARs) are ligand-regulated transcription factors with various important biological effects such as metabolic and cardiovascular physiology. Here, we report the crystal structures of the PPAR alpha ligand-binding domain and PPAR delta ligand-binding domain bound to iloprost, thus providing unambiguous evidence for the direct interaction between iloprost and PPARs and a structural basis for the recognition of PPAR alpha/delta by this prostacyclin analog. In addition to conserved contacts for all PPAR alpha ligands, iloprost also initiates several specific interactions with PPARs using its unique structural groups. Structural and functional studies of receptor-ligand interactions reveal strong functional correlations of the iloprost-PPAR alpha/delta interactions as well as the molecular basis of PPAR subtype selectivity toward iloprost ligand. As such, the structural mechanism may provide a more rational template for designing novel compounds targeting PPARs with more favorable pharmacologic impact based on existing iloprost drugs.zh_CN
dc.description.sponsorshipNational Institutes of Health[DK081757]; American Heart Association; Fundamental Research Funds for the Central Universities[2010121083, 2011121029]; Science Planning Program of Fujian Province[2009J1010]; Office of Science of the United States Department of Energyzh_CN
dc.language.isoenzh_CN
dc.publisherAMER SOC BIOCHEMISTRY MOLECULAR BIOLOGY INCzh_CN
dc.titleStructural Basis for Iloprost as a Dual Peroxisome Proliferator-activated Receptor alpha/delta Agonistzh_CN
dc.typeArticlezh_CN


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