Adamantyl thioureas as soluble epoxide hydrolase inhibitors
A series of inhibitors of the soluble epoxide hydrolase (sEH) containing one or two thiourea groups has been developed. Inhibition potency of the described compounds ranges from 50 μM to 7.2 nM. 1,7-(Heptamethylene)bis[(adamant-1-yl)thiourea] (6f) was found to be the most potent sEH inhibitor, among the thioureas tested.
Vladimir Burmistrov +6 more
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Soluble epoxide hydrolase: Gene structure, expression and deletion [PDF]
Mammalian soluble epoxide hydrolase (sEH) converts epoxides to their corresponding diols through the addition of a water molecule. sEH readily hydrolyzes lipid signaling molecules, including the epoxyeicosatrienoic acids (EETs), epoxidized lipids produced from arachidonic acid by the action of cytochrome p450s.
Todd R, Harris, Bruce D, Hammock
openaire +2 more sources
Synthetic Epoxyeicosatrienoic Acid Mimics Protect Mesangial Cells from Sorafenib-Induced Cell Death
Nineteen potential mimics of 8,9-epoxyeicosatrienoic acid (8,9-EET), a natural bioactive oxylipin, were synthesized and evaluated for their ability to protect renal mesangial cells against sorafenib-induced cell death in a water-soluble tetrazolium (WST ...
Marcus de Bourg +6 more
doaj +1 more source
The role of soluble epoxide hydrolase and its inhibitors in depression
Evidence suggests that around 30 % of patients with depression do not respond to antidepressant treatment, with most of them having sub-chronic levels of inflammation.
Alessandra Borsini
doaj +1 more source
Aryl Hydrocarbon Receptor-Dependent inductions of omega-3 and omega-6 polyunsaturated fatty acid metabolism act inversely on tumor progression. [PDF]
The Western diet contains a high ratio of omega-6 (ω6) to omega-3 (ω3) polyunsaturated fatty acids (PUFA). The prototypical aryl hydrocarbon receptor (AHR) ligand, 2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD), induces CYP1 family enzymes, which can ...
Hammock, Bruce D +5 more
core
Sex-related differences in death control of somatic cells [PDF]
In 2001, The United States Institute of Medicine (IOM) Committee on Understanding the Biology of Sex and Gender Differences concluded that ‘Sex…should be considered when designing and analysing studies in all areas and at all levels of biomedical and ...
FILIPPINI, Antonio +3 more
core +2 more sources
Inhibition of soluble epoxide hydrolase prevents diabetic retinopathy [PDF]
Diabetic retinopathy is an important cause of blindness in adults, and is characterized by progressive loss of vascular cells and slow dissolution of inter-vascular junctions, which result in vascular leakage and retinal oedema. Later stages of the disease are characterized by inflammatory cell infiltration, tissue destruction and neovascularization ...
Hu, Jiong +21 more
openaire +4 more sources
Lysophosphatidic acids are new substrates for the phosphatase domain of soluble epoxide hydrolase
Soluble epoxide hydrolase (sEH) is a bifunctional enzyme that has a C-terminus epoxide hydrolase domain and an N-terminus phosphatase domain. The endogenous substrates of epoxide hydrolase are known to be epoxyeicosatrienoic acids, but the endogenous ...
Ami Oguro, Susumu Imaoka
doaj +1 more source
Integration of the omics data, including metabolomics and proteomics, provides a unique opportunity to search for new associations within metabolic disorders, including Alzheimer’s disease.
Kamil Borkowski +10 more
doaj +1 more source
The precise structures and stereochemistry of trihydroxy-linoleates esterified in human and porcine epidermis and their significance in skin barrier function: Implication of an epoxide hydrolase in the transformations of linoleate [PDF]
Creation of an intact skin water barrier, a prerequisite for life on dry land, requires the lipoxygenase-catalyzed oxidation of the essential fatty acid linoleate, which is esterified to the ω-hydroxyl of an epidermis-specific ceramide.
Boeglin, William E. +5 more
core +1 more source

