• Several members of this group have this metabolic activity on fatty acid epoxides including microsomal epoxide hydrolase (i.e. epoxide hydrolase 1 or EH1), soluble epoxide hydrolase (i.e. epoxide hydrolase 2 or EH2), epoxide hydrolase 3 (EH3), epoxide hydrolase 4 (EH4), and leukotriene A4 hydrolase (see epoxide hydrolase). (wikipedia.org)
  • The soluble EH activity was shown to be distinct from that of the microsomal epoxide hydrolase (mEH) previously discovered with a different substrate selectivity and cellular localization than the mEH. (wikipedia.org)
  • A series of oxetane-containing analogs was studied and we provide the first direct evidence of oxetane hydrolysis by human recombinant microsomal epoxide hydrolase (mEH). (aspetjournals.org)
  • Diol epoxides formed by the sequential action of cytochrome P -450 and the microsomal epoxide hydrolase (mEH) in the endoplasmic reticulum (ER) represent an important class of ultimate carcinogenic metabolites of polycyclic aromatic hydrocarbons. (biochemj.org)
  • Microsomal epoxide hydrolase (mEH, EPHX1) is a critical biotransformation enzyme, catalyzing the metabolism of many xenobiotics. (elsevier.com)
  • Human microsomal epoxide hydrolase (EPHX1) is active in the metabolism of many potentially carcinogenic or otherwise genotoxic epoxides, such as those derived from the oxidation of polyaromatic hydrocarbons. (elsevier.com)
  • To investigate the role of microsomal epoxide hydrolase (mEH) polymorphisms in the aetiology of lung cancer and to assess the interaction between mEH polymorphisms and smoking, we performed a meta-analysis of seven published studies, which included 2078 cases and 3081 controls, and a pooled analysis of eight studies (four published and four unpublished at that time) with a total of 986 cases and 1633 controls. (elsevier.com)
  • Microsomal epoxide hydrolase plays a dual role in the activation and detoxification of carcinogenic compounds. (cumhuriyet.edu.tr)
  • Development of monoclonal antibodies to human microsomal epoxide hydrolase and analysis of "preneoplastic antigen"-like molecules. (jove.com)
  • In case of impaired catalytic activity of a given mutant, the structural integrity of the recombinant enzyme protein was assessed either by its ability to covalently bind the substrate trans-stilbene oxide or by affinity purification on benzyl thio-Sepharose, using the soluble epoxide hydrolase-specific competitive inhibitor 4-fluorochalcone oxide to release the bound enzyme from the affinity matrix. (uzh.ch)
  • AR9281 is a potent and selective inhibitor of soluble epoxide hydrolase (s-EH) , with potential for the treatment of hypertension and type 2 diabetes. (medchemexpress.com)
  • Pharmacokinetics and pharmacodynamics of AR9281, an inhibitor of soluble epoxide hydrolase, in single- and multiple-dose studies in healthy human subjects. (medchemexpress.com)
  • Soluble epoxide hydrolase inhibitor is an inhibitor of soluble epoxide hydrolase , and inhibits human soluble epoxide hydrolase (h-sEH) with pIC 50 of 8.4, extracted from patent WO 2010096722 A1, example 57. (medchemexpress.com)
  • Soluble epoxide hydrolase inhibitor (Example 57) is an inhibitor of soluble epoxide hydrolase, and inhibits human soluble epoxide hydrolase with pIC 50 of 8.4 [1] . (medchemexpress.com)
  • The sEH inhibitory properties of test compounds (including Soluble epoxide hydrolase inhibitor ) are determined using a black 384-well-plate format under the following reaction conditions: 20 mM Tris pH 7.0, 0.1 mM EDTA, 0.1 mg/mL BSA, 5 μM PHOME (substrate), 2 nM sEH enzyme, 1% DMSO (from test compound). (medchemexpress.com)
  • Use of a soluble epoxide hydrolase inhibitor in smoke-induced chronic obstructive pulmonary disease. (curehunter.com)
  • In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor. (axonmedchem.com)
  • Recent insights into the mechanism of epoxide hydrolase activity are combined with these experimental results to support a proposed mechanism of sEH inhibition by chalcone oxides. (elsevier.com)
  • Soluble epoxide hydrolase (sEH) has been proved to be a key enzyme involved in inflammation progression, and inhibition of sEH is therefore very helpful or crucial for the treatment of inflammation-related diseases. (usda.gov)
  • This research group has long-standing experience in delineating the physiological role of an enzyme called soluble epoxide hydrolase (sEH) and inhibition of this enzyme was found to enhance the anti-hypertensive effect of the omega-3-enriched diet. (fatsoflife.com)
  • In contrast, inhibition of soluble epoxide hydrolase by AUDA or TPPU inhibited basal, LPS, IL-1β and PMA induced TNFα release, and LPS-induced NFκB p65 nuclear translocation. (rvc.ac.uk)
  • Biotransformation enzyme that catalyzes the hydrolysis of arene and aliphatic epoxides to less reactive and more water soluble dihydrodiols by the trans addition of water. (abcam.com)
  • Mammalian soluble epoxide hydrolase (sEH) is a member of the α/β-hydrolase fold family of enzymes that catalyzes the hydrolysis of exogenous and endogenous epoxides to vicinal diols. (raw-pharmaceutical-materials.com)
  • Glycoside hydrolases (also called glycosidases or glycosyl hydrolases ) catalyze the hydrolysis of glycosidic bonds in complex sugars . (wikipedia.org)
  • Glycoside hydrolases are classified into EC 3.2.1 as enzymes catalyzing the hydrolysis of O- or S-glycosides. (wikipedia.org)
  • Glycoside hydrolases can also be classified according to the stereochemical outcome of the hydrolysis reaction: thus they can be classified as either retaining or inverting enzymes. (wikipedia.org)
  • Stability : 6 monthsFormulation : TBS buffer at pH 7.4 with 20% glycerolDescription : Mammalian soluble epoxide hydrolase (sEH) is a member of the α/β-hydrolase fold family of enzymes that catalyzes the hydrolysis of exogenous and endogenous epoxides to vicinal diols. (raw-pharmaceutical-materials.com)
  • Furthermore, in [Y378F]LTA4 hydrolase, the value of kcat for epoxide hydrolysis was increased 2.5-fold over that of the wild-type enzyme. (ox.ac.uk)
  • In enzyme science , Hydrolases (Hydrolase Enzymes) , as hydrolysis reactions , are a group of broad Top-level Enzyme Reactions (Enzyme Catalysts) , involved with the formation of two products from a substrate by hydrolysis , in the Top-level Enzyme Reaction Group EC 3. (wellnessadvocate.com)
  • In our body, a Hydrolases (Hydrolase Enzyme) is an enzyme that catalyzes the hydrolysis of a chemical bond. (wellnessadvocate.com)
  • In enzyme science , Glycosidases (Glycoside Hydrolases) are glycosylase enzymes in the hydrolase enzyme class , that catalyze the hydrolysis and/or rearrangement of the glycosidic linkage to release smaller sugars. (wellnessadvocate.com)
  • Glycosidases (Glycoside Hydrolases) , as enzymes, catalyze the hydrolysis of either O-glycosides or S-glycosides. (wellnessadvocate.com)
  • Glycoside hydrolases can catalyze the hydrolysis of O-, N- and S-linked glycosides. (wellnessadvocate.com)
  • In enzyme science, Acid Anhydride Hydrolases are a class of hydrolase enzyme reactions that catalyze the hydrolysis of a acid anhydride bond. (wellnessadvocate.com)
  • Variations in the human soluble epoxide hydrolase gene and recurrence of atrial fibrillation after catheter ablation. (jove.com)
  • The sEH was first identified in the cytosolic fraction of mouse liver through its activity on epoxide containing substrates such as juvenile hormone and lipid epoxides such as epoxystearate. (wikipedia.org)
  • This work defines oxetanes as the first nonepoxide class of substrates for human mEH, which was previously known to catalyze the hydrolytic ring opening of electrophilic and potentially toxic epoxide-containing drugs, drug metabolites, and exogenous organochemicals. (aspetjournals.org)
  • Of the 10 different EH substrates that were tested, Hv-mEH1 showed the highest specific activity (1180 nmol min -1 mg -1 ) for a 1,2-disubstituted epoxide-containing fluorescent substrate. (elsevier.com)
  • Enzymatic profiles were evaluated with cis-stilbene oxide (cSO) and benzo[a]pyrene-4,5-epoxide (BaPO), two prototypical substrates for the hydrolase. (elsevier.com)
  • In enzymology, a hepoxilin-epoxide hydrolase (EC 3.3.2.7) is an enzyme that catalyzes the conversion of the epoxyalcohol metabolites arachidonic acid, hepoxilin A3 and hepoxilin B3 to their tri-hydroxyl products, trioxolin A3 and trioxilin B3, respectively. (wikipedia.org)
  • Other names in common use include hepoxilin epoxide hydrolase, hepoxylin hydrolase, and hepoxilin A3 hydrolase. (wikipedia.org)
  • Since the hepoxilins are metabolites of arachidonic acid, hepoxilin-epoxide hydrolase participates in arachidonic acid metabolism. (wikipedia.org)
  • Soluble epoxide hydrolase is widely expressed in a diversity of human and other mammal tissues and therefore appears to be the hepoxilin hydrolase responsible for inactivating hepoxilin A3 and B3 (see soluble epoxide hydrolase#Function and epoxide hydrolase#Hepoxilin-epoxide hydrolase). (wikipedia.org)
  • The other fatty acid epoxide hydrolases cited in the Epoxide hydrolases section (above) have not be reported for hepoxilin-epoxide hydrolase activity, could possibly exhibit this, and therefore contribute to inactivating the hepoxilins. (wikipedia.org)
  • Recombinant fragment, corresponding to a region within amino acids 1-193 of Human Epoxide hydrolase (NP_000111). (abcam.com)
  • Disclosed are sulfone compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. (sumobrain.com)
  • A series of substituted chalcone oxides (1,3-diphenyl-2-oxiranyl propanones) and structural analogs was synthesized to investigate the mechanism by which they inhibit soluble epoxide hydrolases (sEH). (elsevier.com)
  • The rats were treated with N-methylsulfonyl-12,12-dibromododec-11-enamide to inhibit 20-HETE formation and/or with N-cyclohexyl-N-dodecyl urea to inhibit soluble epoxide hydrolase and prevent degradation of EETs. (curehunter.com)
  • Epoxide hydrolases represent a group of enzymes that convert various types of epoxides to vicinal diols. (wikipedia.org)
  • This enzyme, found in both the cytosol and peroxisomes, binds to specific epoxides and converts them to the corresponding diols. (wikipedia.org)
  • sEH converts epoxides, or three membered cyclic ethers, to their corresponding diols through the addition of a molecule of water. (wikipedia.org)
  • The resulting diols are more water-soluble than the parent epoxides, and so are more readily excreted by the organism. (wikipedia.org)
  • These endogenous lipid mediators are converted into inactive diols by soluble epoxide hydrolase (sEH), and so inhibiting this enzyme would be expected to enhance the stability and therapeutic actions of EETs [ 17 ]. (hindawi.com)
  • The soluble epoxide hydrolase (sEH), which is expressed in pulmonary artery smooth muscle cells, metabolizes cytochrome P450 (CYP) epoxygenase-derived epoxyeicosatrienoic acids (EETs) to their less active diols. (ahajournals.org)
  • Epoxide hydrolases (EHs) are α/β-hydrolase fold superfamily enzymes that convert epoxides to 1,2-trans diols. (elsevier.com)
  • Hydration of EETs by the soluble epoxide hydrolase (sEH) is the major route of their degradation to the less bioactive diols. (elsevier.com)
  • In enzyme science , Peptide Hydrolases (Peptidases) , aka Proteases (Proteolytic Enzymes) , are hydrolases that specifically cleave the peptide bonds found in proteins and peptides . (wellnessadvocate.com)
  • The C-term-EH catalyzes the addition of water to an epoxide to yield a vicinal diol (reaction 1). (wikipedia.org)
  • A ) Fatty acid epoxide and diol levels in retinas from WT and sEH -/- mice exposed to normoxia (21% O 2 ) or hyperoxia (75% O 2 ) for 24 hours starting on P7. (jci.org)
  • Biological transformation of PUFA through CYP-mediated hydroxylation, epoxidation, and allylic oxidation produces lipid mediators, which may be subsequently hydrolyzed to corresponding diol metabolites by soluble epoxide hydrolase (sEH). (frontiersin.org)
  • Aim: To assess the association between human epoxide hydrolase exon 3 and 4 polymorphisms and pre-eclampsia by carrying out a case-control study in Turkish women. (cumhuriyet.edu.tr)
  • Despite a very high functional diversity within the α/β-hydrolase fold superfamily the enzymes within that class show very high structural homology. (uni-greifswald.de)
  • The form of sEH in the intracellular environment is a homodimer with two distinct activities in two separate structural domains of each monomer: the C-terminal epoxide hydrolase activity (soluble epoxide hydrolase: EC 3.3.2.10) and the N-terminal phosphatase activity (lipid-phosphate phosphatase: EC 3.1.3.76). (wikipedia.org)
  • EC 3.3.2.10) is a key enzyme in the metabolism of eicosanoid epoxides, including epoxyeicosatrienoic acids (EETs) and of leukotoxin (LTX). (axonmedchem.com)
  • Conversely, the sEH plays a major role in the in vivo metabolism of endogenous lipid epoxides, such as the EETs and squalene oxide, a key intermediate in the synthesis of cholesterol. (wikipedia.org)
  • Epoxide hydrolases (EHs) are enzymes involved in the metabolism of endogenous and exogenous epoxides, and the development of EH inhibitors has important applications in the medicine. (usda.gov)
  • By reducing sEH epoxide hydrolase activity, and thereby shutting off the major route of metabolism of the EETs, the levels of these molecules can be stabilized or increased, increasing blood flow and reducing hypertension. (wikipedia.org)
  • Epoxyeicosatrienoic acids (EETs) are products of CYP450 epoxygenase and are degraded to DHETs by soluble epoxide hydrolase (sEH). (ahajournals.org)
  • Studies using a lipid epoxide as a substrate detected this activity in the soluble fraction of multiple organs, though at a lesser amount than in liver and kidney. (wikipedia.org)
  • Thus, compared with soybean EH, the active site of rat liver soluble EH displays a very distinct means of anchoring the oxirane ring of the fatty acid epoxides, and therefore appears to be a poor model for mapping the catalytic domain of plant EHs. (biochemj.org)
  • The ability of Hv-mEH1 to rapidly hydrolyze 1,2-disubstituted epoxides suggests that it may play roles in the metabolism of fatty acid epoxides such as those that are commonly found in the diet of Heliothis. (elsevier.com)
  • Chosen library residues do also influence selectivity and activity for other structurally similar epoxides styrene oxide ( 2 ), trans -2-methyl styrene oxide ( 3 ) and trans -stilbene oxide ( 5 ), despite these not being selected for. (diva-portal.org)
  • Soluble epoxide hydrolase (sEH) is a bifunctional enzyme that in humans is encoded by the EPHX2 gene. (wikipedia.org)
  • The ability of EH1, EH3, EH4, and leukotriene A4 hydrolase to metabolize hepoxilins to trioxilins has not yet been reported. (wikipedia.org)
  • Leukotriene A4 hydrolase , also known as LTA4H is a human gene . (wikipedia.org)
  • Other names in common use include LTA4 hydrolase , LTA4H , and leukotriene A4 hydrolase . (wikipedia.org)
  • Molecular cloning of a cDNA coding for human leukotriene A4 hydrolase. (wikipedia.org)
  • Leukotriene A4 hydrolase in the human lung. (wikipedia.org)
  • Leukotriene A4 hydrolase: protection from mechanism-based inactivation by mutation of tyrosine-378. (ox.ac.uk)
  • Soluble epoxide hydrolase (i.e. epoxide hydrolase 2 or EH2) sEH also appears to be the hepoxilin hydrolase that is responsible for inactivating the epoxyalcohol metabolites of arachidonic acid, hepoxilin A3 and hepoxiin B3. (wikipedia.org)
  • Given that DHA metabolism by cytochrome P450 and soluble epoxide hydrolase (sEH) enzymes affects retinal angiogenesis and vascular stability, we investigated the role of sEH in a mouse model of ROP. (jci.org)
  • Incubations with human liver fractions and hepatocytes were performed with and without inhibitors of cytochrome P450 (P450), mEH and soluble epoxide hydrolase (sEH). (aspetjournals.org)
  • In higher organisms glycoside hydrolases are found within the endoplasmic reticulum and Golgi apparatus where they are involved in processing of N-linked glycoproteins , and in the lysosome as enzymes involved in the degradation of carbohydrate structures. (wikipedia.org)
  • This study investigated the hypothesis that inhibiting soluble epoxide hydrolase (sEH), responsible for converting epoxyeicosatrienoic acids to dihydroxyeicosatrienoic acids protects mitochondrial from injury caused by myocardial infarction. (frontiersin.org)
  • We have evaluated the performance of standard rigid(receptor)/flexible(ligand) docking approaches with respect to last-generation fully flexible docking methods to obtain reasonable poses in a very challenging case: soluble Epoxide Hydrolase (sEH), a flexible protein showing different binding sites. (upc.edu)
  • Human endothelial cells expressed CYP2J2 and soluble epoxide hydrolase (sEH) mRNA and protein. (rvc.ac.uk)
  • LTA4 hydrolase/aminopeptidase is suicide inactivated during catalysis via an apparently mechanism-based irreversible binding of LTA4 to the protein in a 1:1 stoichiometry. (ox.ac.uk)
  • Previously, we have identified a henicosapeptide, encompassing residues Leu-365 to Lys-385 in human LTA4 hydrolase, which contains a site involved in the covalent binding of LTA4 to the native enzyme. (ox.ac.uk)
  • Canadian implantable defibrillator study (ClDS) a randomized trial of the implantable cardioverter defibrillator against Otorex Drops 10`ML. Seidegard J, DePierre JW and Pero RW ф1984) Otorex Drops 10`ML and characterisation of membrane- bound and soluble epoxide hydrolase activities in resting mononuclear leukocytes from human blood. (underfoot.ru)
  • The C-terminal domain is responsible for the epoxide hydrolase activity while the N-terminal domain has a catalytic center with phosphatase activity. (raw-pharmaceutical-materials.com)
  • The predicted amino acid residues were exchanged by site-directed mutagenesis of the epoxide hydrolase cDNA, followed by the expression of the respective mutant enzymes in Escherichia coli. (uzh.ch)
  • Thus, by a single-point mutation in LTA4 hydrolase, catalysis and covalent modification/inactivation have been dissociated, yielding an enzyme with increased turnover and resistance to mechanism-based inactivation. (ox.ac.uk)
  • 14, 61-71) we selected candidate amino acid residues for the putative catalytic triad of the rat soluble epoxide hydrolase. (uzh.ch)
  • Recent studies show increased activity of soluble epoxide hydrolase (sEH) during obesity and metabolic dysfunction. (hindawi.com)
  • Accordingly, the soluble epoxide hydrolase metabolic pathway is considered to function in vivo to inactivate or limit the activity of the hepoxilins. (wikipedia.org)
  • A total of 25 different mutants were analyzed for their epoxide hydrolase activity toward the model substrate trans-stilbene oxide. (uzh.ch)
  • Epoxide hydrolase I from Solanum tuberosum (StEH1) and isolated variants thereof has been studied for mapping structure-function relationships with the ultimate goal of being able to in silico predict modifications needed for a certain activity or selectivity. (diva-portal.org)
  • The isolated hits were used to study varying selectivity and activity with different epoxides. (diva-portal.org)