ArticleThe Journal of biological chemistry2011
Structural basis for iloprost as a dual peroxisome proliferator-activated receptor alpha/delta agonist.
Article in The Journal of biological chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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Who cites it
14 citing papers in PubMed, 29 citations in OpenAlex.
- Effects ofInternational journal of molecular sciences · 2026Article
- Current Overview of the Biology and Pharmacology in Sugen/Hypoxia-Induced Pulmonary Hypertension in Rats.Journal of aerosol medicine and pulmonary drug delivery · 2024Review
- Co-Incubation with PPARβ/δ Agonists and Antagonists Modeled Using Computational Chemistry: Effect on LPS Induced Inflammatory Markers in Pulmonary Artery.International journal of molecular sciences · 2021Article
- Elucidation of Molecular Mechanism of a Selective PPARα Modulator, Pemafibrate, through Combinational Approaches of X-ray Crystallography, Thermodynamic Analysis, and First-Principle Calculations.International journal of molecular sciences · 2020Article
- Arjunolic acid, a peroxisome proliferator-activated receptor α agonist, regresses cardiac fibrosis by inhibiting non-canonical TGF-β signaling.The Journal of biological chemistry · 2017Article
- The expansive role of oxylipins on platelet biology.Journal of molecular medicine (Berlin, Germany) · 2017Review
- Role of prostacyclin signaling in endothelial production of soluble amyloid precursor protein-α in cerebral microvessels.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2017Article
- Activation of PPARδ: from computer modelling to biological effects.British journal of pharmacology · 2015Review
- Structure-based virtual screening and discovery of New PPARδ/γ dual agonist and PPARδ and γ agonists.PloS one · 2015Article
- ROR nuclear receptors: structures, related diseases, and drug discovery.Acta pharmacologica Sinica · 2015Review
- Targeting nuclear receptors with marine natural products.Marine drugs · 2014Review
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- Article
- Vascular effects of prostacyclin: does activation of PPARδ play a role?Trends in pharmacological sciences · 2012Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
Abstract
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 PPARα ligand-binding domain and PPARδ 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 PPARα/δ by this prostacyclin analog. In addition to conserved contacts for all PPARα 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-PPARα/δ 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.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.