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	Structural Basis for Iloprost as a Dual Peroxisome Proliferator-activated Receptor alpha/delta Agonist
	Li, Yong ; Li Y(李勇) ; Jin, Lihua ; Jin LH(金利华) ; Lin, Shengchen ; Rong, Hui ; Zheng, Songyang ; Jin, Shikan ; Wang, Rui
	2011-07-20
英文摘要	Iloprost 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.; National 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 Energy
语种	英语
出版者	AMER SOC BIOCHEMISTRY MOLECULAR BIOLOGY INC
内容类型	期刊论文
源URL	[http://dx.doi.org/doi:10.1074/jbc.M111.266023]
专题	生命科学－已发表论文
推荐引用方式 GB/T 7714	Li, Yong,Li Y,Jin, Lihua,et al. Structural Basis for Iloprost as a Dual Peroxisome Proliferator-activated Receptor alpha/delta Agonist[J],2011.
APA	Li, Yong.,李勇.,Jin, Lihua.,金利华.,Lin, Shengchen.,...&Wang, Rui.(2011).Structural Basis for Iloprost as a Dual Peroxisome Proliferator-activated Receptor alpha/delta Agonist..
MLA	Li, Yong,et al."Structural Basis for Iloprost as a Dual Peroxisome Proliferator-activated Receptor alpha/delta Agonist".(2011).

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