A high-throughput mass spectrometric assay for discovery of human lipoxygenase inhibitors and allosteric effectors. [PDF]
Anal Biochem, 2015 Lipoxygenases (LOXs) regulate inflammation through the production of a variety of molecules whose specific downstream effects are not entirely understood due to the complexity of the inflammation pathway.
Holman, Theodore R +2 more
core +2 more sources
α-Conotoxins Enhance both the In Vivo Suppression of Ehrlich carcinoma Growth and In Vitro Reduction in Cell Viability Elicited by Cyclooxygenase and Lipoxygenase Inhibitors [PDF]
Marine Drugs, 2020 Several biochemical mechanisms, including the arachidonic acid cascade and activation of nicotinic acetylcholine receptors (nAChRs), are involved in increased tumor survival. Combined application of inhibitors acting on these two pathways may result in a
Alexey V. Osipov +6 more
doaj +2 more sources
A fluorescence-based assay for measuring the redox potential of 5-lipoxygenase inhibitors. [PDF]
PLoS ONE, 2014 The activities and side effects of 5-lipoxygenase (5-LO) inhibitors can be predicted by identifying their redox mechanisms. In this study, we developed a fluorescence-based method to measure the redox potential of 5-LO inhibitors and compared it to the ...
Sangchul Lee +3 more
doaj +2 more sources
Microwave Assisted Synthesis of Antioxidant Dihydro-Pyrazole Hybrids as Possible Lipoxygenase Inhibitors [PDF]
MoleculesFree radicals and inflammation have pivotal role in various degenerative diseases like cancer, rheumatoid arthritis, diabetes, cardiovascular and neurodegenerative disorders.
Stergiani-Chrysovalanti Peitzika +2 more
doaj +2 more sources
Design, synthesis, and computational studies on dihydropyrimidine scaffolds as potential lipoxygenase inhibitors and cancer chemopreventive agents [PDF]
Drug Design, Development and Therapy, 2015 Katharigatta N Venugopala,1,2 Reshme Govender,2 Mohammed A Khedr,1,3 Rashmi Venugopala,4 Bandar E Aldhubiab,1 Sree Harsha,1 Bharti Odhav2 1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Kingdom of ...
Venugopala KN +6 more
doaj +2 more sources
Infectious agents in atherosclerotic cardiovascular diseases through oxidative stress [PDF]
, 2017 Accumulating evidence demonstrates that vascular oxidative stress is a critical feature of atherosclerotic process, potentially triggered by several infectious agents that are considered as risk co-factors for the atherosclerotic cardiovascular diseases (
Di Pietro, M +4 more
core +5 more sources
Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase. [PDF]
, 2009 Pharmacological suppression of leukotriene biosynthesis by inhibitors of 5-lipoxygenase (5-LO) is a strategy to intervene with inflammatory and allergic disorders.
BÜHRING U +8 more
core +1 more source
Involvement of leukotriene pathway in the pathogenesis of ischemia-reperfusion injury and septic and non-septic shock. [PDF]
, 2009 The 5-lipoxygenase (5-LO) pathway is responsible for the production of leukotrienes (LTs), inflammatory lipid mediators which play a role in innate immunity. More recently, a pivotal role of LTs in ischemia-reperfusion and shock injury has been suggested.
CUZZOCREA S +2 more
core +1 more source
Trichostatin A induces 5-lipoxygenase promoter activity and mRNA expression via inhibition of histone deacetylase 2 and 3 [PDF]
, 2012 The 5-lipoxygenase (5-LO) is the key enzyme in the formation of leukotrienes. We have previously shown that the histone deacetylase (HDAC) inhibitor trichostatin A (TSA) activates 5-LO transcription via recruitment of Sp1, Sp3 and RNA polymerase II to ...
Grez, Manuel +6 more
core +1 more source
Hepatology, EarlyView., 2022 CHIN117 is a dual cysteinyl leukotriene receptor 1 (CYSLTR1) antagonist and G‐protein‐coupled bile acid receptor 1 (GPBAR1) agonist. In the liver, GPBAR1 and CYSLTR1 are coexpressed by liver sinusoidal endothelial cells (LSECs), HSCs, circulating monocytes/macrophages, and liver resident macrophages (Kupffer cells).
Michele Biagioli +13 more
wiley +1 more source