ArticleNature chemical biology2020
Structural and mechanistic insights into 5-lipoxygenase inhibition by natural products.
Article in Nature chemical biology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 107 papers.
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Who cites it
107 citing papers in PubMed, 211 citations in OpenAlex.
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- 7-O-methylpunctatin is a potential inhibitor of human arachidonate 5-lipoxygenase: molecular and structural insights into anti-atherosclerosis therapeutics.Molecular diversity · 2026Article
- An In Silico Study of Resveratrol Derivatives as Dual Inhibitors of Cyclooxygenase-2 (COX-2) and 5-Lipoxygenase (5-LOX) in Cancer Therapy.Biotechnology and applied biochemistry · 2026Article
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- Cassipourol and β-sitosterol from Malva parviflora L.: a mechanistic study of dual anti-inflammatory action against COX/LOX and TNF-α/BCL-2.Scientific reports · 2026Article
- Experimental Characterization Combined with Computational Network Analysis of Metabolites Associated with Chrysanthemum morifolium-derived exosome-like Nanoparticles in Predicting Potential AKI-relevant Targets.Cell biochemistry and biophysics · 2026Article
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- Resolvin D5 Inhibits CXCL8 Expression in Colonic Epithelial Cells Through Activating GPR101 to Impede Neutrophil Recruitment and Consequently Alleviate Ulcerative Colitis.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- A Multistep Computational Approach to Achieve a Complete Human 5-Lipoxygenase Structure and Provide a Pharmacophore Model for Further Drug Design.Molecular informatics · 2026Article
- Dual Inhibition of COX-2/5-LOX Through Novel Hybrids of NSAIDs and Peptides: Insights from Molecular Dynamics Simulation and Per-Residue Decomposition.ChemistryOpen · 2026Article
- Design, Synthesis, and In Vitro Enzymatic Evaluation of Novel Flavone Derivatives as Dual COX-2/5-LOX Inhibitors Supported by Molecular Docking and ADMET Analysis.Current issues in molecular biology · 2026Article
- Exploring the impact of the innovative compound 3-(3-(4-hydroxy-2-oxo-2H-chromen-3-yl)-5-(pyridin-3-yl)-1H-pyrazol-1-yl) indolin-2-one on accelerating wound recovery.Scientific reports · 2026Article
- Acetyl-11-keto-β-boswellic acid attenuates tau oligomer-induced neurotoxicity in neuroblastoma cell model.BMC neuroscience · 2026Article
47 more citing papers are in PubMed but not listed here.
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8 authors at 3 institutions in 2 countries.
Funding
Abstract
Leukotrienes (LT) are lipid mediators of the inflammatory response that are linked to asthma and atherosclerosis. LT biosynthesis is initiated by 5-lipoxygenase (5-LOX) with the assistance of the substrate-binding 5-LOX-activating protein at the nuclear membrane. Here, we contrast the structural and functional consequences of the binding of two natural product inhibitors of 5-LOX. The redox-type inhibitor nordihydroguaiaretic acid (NDGA) is lodged in the 5-LOX active site, now fully exposed by disordering of the helix that caps it in the apo-enzyme. In contrast, the allosteric inhibitor 3-acetyl-11-keto-beta-boswellic acid (AKBA) from frankincense wedges between the membrane-binding and catalytic domains of 5-LOX, some 30 Å from the catalytic iron. While enzyme inhibition by NDGA is robust, AKBA promotes a shift in the regiospecificity, evident in human embryonic kidney 293 cells and in primary immune cells expressing 5-LOX. Our results suggest a new approach to isoform-specific 5-LOX inhibitor development through exploitation of an allosteric site in 5-LOX.
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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.