ArticleScientific reports2017
Pharmacological profile and efficiency in vivo of diflapolin, the first dual inhibitor of 5-lipoxygenase-activating protein and soluble epoxide hydrolase.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 49 citations in OpenAlex.
- Reorganization of Innate Immune Cell Lipid Profiles by Bioinspired Meroterpenoids to Limit Inflammation.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Effective Therapeutic Strategies to Prevent Frailty and Falls in Community-Dwelling Older Adults.Aging and disease · 2025Review
- Role of the soluble epoxide hydrolase in keratinocyte proliferation and sensitivity of skin to inflammatory stimuli.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2024Article
- Modulation of the 5-Lipoxygenase Pathway by Chalcogen-Containing Inhibitors of Leukotriene AInternational journal of molecular sciences · 2023Article
- Differential impact of 5-lipoxygenase-activating protein antagonists on the biosynthesis of leukotrienes and of specialized pro-resolving mediators.Frontiers in pharmacology · 2023Article
- Synthesis and structure-activity relationships for some novel diflapolin derivatives with benzimidazole subunit.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Development of SFC-MS Method for Quantification of Eicosanoids Biosynthesized in Primary Human Blood Cells.Metabolites · 2022Article
- Article
- Review
- Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation.Journal of medicinal chemistry · 2021Article
- From Vietnamese plants to a biflavonoid that relieves inflammation by triggering the lipid mediator class switch to resolution.Acta pharmaceutica Sinica. B · 2021Article
- Discovery of Soluble Epoxide Hydrolase Inhibitors from Chemical Synthesis and Natural Products.Journal of medicinal chemistry · 2021Review
- Mitochondria Are Potential Targets for the Development of New Drugs Against Neutrophilic Inflammation in Severe Pneumonia Including COVID-19.Frontiers in pharmacology · 2021Article
- Small Molecule Soluble Epoxide Hydrolase Inhibitors in Multitarget and Combination Therapies for Inflammation and Cancer.Molecules (Basel, Switzerland) · 2020Review
- Exotoxins from Staphylococcus aureus activate 5-lipoxygenase and induce leukotriene biosynthesis.Cellular and molecular life sciences : CMLS · 2020Article
- Novel Analgesics with Peripheral Targets.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2020Review
- Computer-Aided Fragment Growing Strategies to Design Dual Inhibitors of Soluble Epoxide Hydrolase and LTA4 Hydrolase.ACS medicinal chemistry letters · 2020Article
- Design of Dual Inhibitors of Soluble Epoxide Hydrolase and LTAACS medicinal chemistry letters · 2020Article
- Development of multitarget agents possessing soluble epoxide hydrolase inhibitory activity.Prostaglandins & other lipid mediators · 2019Review
- Synthesis, Biological Evaluation and Structure-Activity Relationships of Diflapolin Analogues as Dual sEH/FLAP Inhibitors.ACS medicinal chemistry letters · 2019Article
Corrections and comments
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Authors and funding
17 authors at 5 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Arachidonic acid (AA) is metabolized to diverse bioactive lipid mediators. Whereas the 5-lipoxygenase-activating protein (FLAP) facilitates AA conversion by 5-lipoxygenase (5-LOX) to pro-inflammatory leukotrienes (LTs), the soluble epoxide hydrolase (sEH) degrades anti-inflammatory epoxyeicosatrienoic acids (EETs). Accordingly, dual FLAP/sEH inhibition might be advantageous drugs for intervention of inflammation. We present the in vivo pharmacological profile and efficiency of N-[4-(benzothiazol-2-ylmethoxy)-2-methylphenyl]-N'-(3,4-dichlorophenyl)urea (diflapolin) that dually targets FLAP and sEH. Diflapolin inhibited 5-LOX product formation in intact human monocytes and neutrophils with IC
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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.