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Literature summary for 3.3.2.10 extracted from

  • Iliff, J.J.; Alkayed, N.J.
    Soluble epoxide hydrolase inhibition: targeting multiple mechanisms of ischemic brain injury with a single agent (2009), Future Neurol., 4, 179-199.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine sEH is a potential therapeutic target in the treatment of ischemic stroke Rattus norvegicus
medicine sEH is a potential therapeutic target in the treatment of ischemic stroke. Treatment of acute ischemic stroke with sEH inhibition, overview Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
gene ephx2 Homo sapiens

Protein Variants

Protein Variants Comment Organism
C154Y a naturally occuring polymorphism, the substitutions results in an enzyme with increased epoxide hydrolase activity, the mutation is associated with with ischemic stroke risk Homo sapiens
E470G a naturally occuring polymorphism, the substitutions results in an enzyme with increased epoxide hydrolase activity, the mutation is associated with with ischemic stroke risk Homo sapiens
K55R a naturally occuring polymorphism, the substitutions results in an enzyme with increased epoxide hydrolase activity, the mutation is associated with with ischemic stroke risk Homo sapiens
additional information gene EPHX2 contains several naturally occuring polymorphisms within study populations, some of which resulted in non-synonymous amino acid substitutions Homo sapiens
R287Q a naturally occuring polymorphism, the substitutions results in an enzyme with reduced epoxide hydrolase activity Homo sapiens
S402R a naturally occuring polymorphism, the substitutions results in an enzyme with reduced epoxide hydrolase activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
12-(3-adamantan-1-yl-ureido)dodecanoic acid AUDA Homo sapiens
12-(3-adamantan-1-yl-ureido)dodecanoic acid AUDA Mus musculus
12-(3-adamantan-1-yl-ureido)dodecanoic acid AUDA Rattus norvegicus
12-(3-adamantan-1-yl-ureido)dodecanoic acid butyl ester AUDA-BE, displays improved bioavailability compared to AUDA Homo sapiens
12-(3-adamantan-1-yl-ureido)dodecanoic acid butyl ester AUDA-BE, displays improved bioavailability compared to AUDA, can be administered ip to improve stroke outcome in a mouse model of ischemia/reperfusion injury Mus musculus
12-(3-adamantan-1-yl-ureido)dodecanoic acid butyl ester AUDA-BE Rattus norvegicus
dicyclohexylurea
-
Homo sapiens
dicyclohexylurea
-
Mus musculus
dicyclohexylurea
-
Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
soluble
-
Mus musculus
-
-
soluble
-
Homo sapiens
-
-
soluble
-
Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
(5Z,11Z,14Z)-8,9-epoxyeicosatrienoic acid + H2O Mus musculus
-
(5Z,11Z,14Z)-8,9-dihydroxyeicosatrienoic acid
-
?
(5Z,11Z,14Z)-8,9-epoxyeicosatrienoic acid + H2O Homo sapiens
-
(5Z,11Z,14Z)-8,9-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,11Z)-14,15-epoxyeicosatrienoic acid + H2O Mus musculus
-
(5Z,8Z,11Z)-14,15-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,11Z)-14,15-epoxyeicosatrienoic acid + H2O Homo sapiens
-
(5Z,8Z,11Z)-14,15-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,11Z)-14,15-epoxyeicosatrienoic acid + H2O Rattus norvegicus EETs exhibit a wide array of potentially beneficial actions in stroke, including vasodilation, neuroprotection, promotion of angiogenesis and suppression of platelet aggregation, oxidative stress and postischemic inflammation (5Z,8Z,11Z)-14,15-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,14Z)-11,12-epoxyeicosatrienoic acid + H2O Mus musculus
-
(5Z,8Z,14Z)-11,12-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,14Z)-11,12-epoxyeicosatrienoic acid + H2O Homo sapiens
-
(5Z,8Z,14Z)-11,12-dihydroxyeicosatrienoic acid
-
?
(8Z,11Z,14Z)-5,6-epoxyeicosatrienoic acid + H2O Mus musculus
-
(8Z,11Z,14Z)-5,6-dihydroxyeicosatrienoic acid
-
?
(8Z,11Z,14Z)-5,6-epoxyeicosatrienoic acid + H2O Homo sapiens
-
(8Z,11Z,14Z)-5,6-dihydroxyeicosatrienoic acid
-
?
additional information Mus musculus EETs are important regulators of cardiovascular function, of cerebral blood flow, and exhibit a wide array of potentially beneficial actions in stroke, including vasodilation, neuroprotection, promotion of angiogenesis and suppression of platelet aggregation, oxidative stress and postischemic inflammation, detailed overview ?
-
?
additional information Homo sapiens EETs are important regulators of cardiovascular function, of cerebral blood flow, and exhibit a wide array of potentially beneficial actions in stroke, including vasodilation, neuroprotection, promotion of angiogenesis and suppression of platelet aggregation, oxidative stress and postischemic inflammation, detailed overview ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P34913 gene EPHX2
-
Mus musculus P34914 gene EPHX2
-
Rattus norvegicus P80299 gene EPHX2
-

Source Tissue

Source Tissue Comment Organism Textmining
brain in vascular smooth muscle and endothelial cell layers, in white matter Homo sapiens
-
brain in vascular smooth muscle and endothelial cell layersm in white matter. sEH in rodent brain is neither vascular nor glial, but rather neuronal. In brain parenchymal tissue, sEH is markedly expressed in neuronal cell bodies and processes, particularly within the cerebral cortex and striatum Mus musculus
-
brain cortex
-
Mus musculus
-
corpus striatum
-
Mus musculus
-
glia restricted primarily to oligodendrocytes in the white matter Homo sapiens
-
kidney
-
Mus musculus
-
kidney
-
Homo sapiens
-
liver
-
Mus musculus
-
liver
-
Homo sapiens
-
U-937 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(5Z,11Z,14Z)-8,9-epoxyeicosatrienoic acid + H2O
-
Mus musculus (5Z,11Z,14Z)-8,9-dihydroxyeicosatrienoic acid
-
?
(5Z,11Z,14Z)-8,9-epoxyeicosatrienoic acid + H2O
-
Homo sapiens (5Z,11Z,14Z)-8,9-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,11Z)-14,15-epoxyeicosatrienoic acid + H2O
-
Mus musculus (5Z,8Z,11Z)-14,15-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,11Z)-14,15-epoxyeicosatrienoic acid + H2O
-
Homo sapiens (5Z,8Z,11Z)-14,15-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,11Z)-14,15-epoxyeicosatrienoic acid + H2O
-
Rattus norvegicus (5Z,8Z,11Z)-14,15-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,11Z)-14,15-epoxyeicosatrienoic acid + H2O EETs exhibit a wide array of potentially beneficial actions in stroke, including vasodilation, neuroprotection, promotion of angiogenesis and suppression of platelet aggregation, oxidative stress and postischemic inflammation Rattus norvegicus (5Z,8Z,11Z)-14,15-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,14Z)-11,12-epoxyeicosatrienoic acid + H2O
-
Mus musculus (5Z,8Z,14Z)-11,12-dihydroxyeicosatrienoic acid
-
?
(5Z,8Z,14Z)-11,12-epoxyeicosatrienoic acid + H2O
-
Homo sapiens (5Z,8Z,14Z)-11,12-dihydroxyeicosatrienoic acid
-
?
(8Z,11Z,14Z)-5,6-epoxyeicosatrienoic acid + H2O
-
Mus musculus (8Z,11Z,14Z)-5,6-dihydroxyeicosatrienoic acid
-
?
(8Z,11Z,14Z)-5,6-epoxyeicosatrienoic acid + H2O
-
Homo sapiens (8Z,11Z,14Z)-5,6-dihydroxyeicosatrienoic acid
-
?
additional information EETs are important regulators of cardiovascular function, of cerebral blood flow, and exhibit a wide array of potentially beneficial actions in stroke, including vasodilation, neuroprotection, promotion of angiogenesis and suppression of platelet aggregation, oxidative stress and postischemic inflammation, detailed overview Mus musculus ?
-
?
additional information EETs are important regulators of cardiovascular function, of cerebral blood flow, and exhibit a wide array of potentially beneficial actions in stroke, including vasodilation, neuroprotection, promotion of angiogenesis and suppression of platelet aggregation, oxidative stress and postischemic inflammation, detailed overview Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
SEH
-
Mus musculus
SEH
-
Homo sapiens
SEH
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000003
-
-
Rattus norvegicus dicyclohexylurea
0.000007
-
-
Rattus norvegicus 12-(3-adamantan-1-yl-ureido)dodecanoic acid butyl ester

General Information

General Information Comment Organism
malfunction polymorphimsm in gene EPHX2 are associated with ischemic stroke risk. sEH inhibition and gene deletion reduce infarct size after focal cerebral ischemia in mice Mus musculus
malfunction polymorphimsm in gene EPHX2 are associated with ischemic stroke risk. sEH inhibition and gene deletion reduce infarct size after focal cerebral ischemia in mice Homo sapiens
malfunction polymorphimsm in gene EPHX2 are associated with ischemic stroke risk. sEH inhibition and gene deletion reduce infarct size after focal cerebral ischemia in mice Rattus norvegicus
additional information enzyme inhibition protects against ischemic stroke, mechanism and cytoprotective, anti-inflammatory, and other effects, overview Mus musculus
additional information enzyme inhibition protects against ischemic stroke, mechanism and cytoprotective, anti-inflammatory, and other effects, overview Homo sapiens
physiological function soluble epoxide hydrolase is a key enzyme in the metabolic conversion and degradation of P450 eicosanoids called epoxyeicosatrienoic acids, EETs Mus musculus
physiological function soluble epoxide hydrolase is a key enzyme in the metabolic conversion and degradation of P450 eicosanoids called epoxyeicosatrienoic acids, EETs Homo sapiens
physiological function soluble epoxide hydrolase is a key enzyme in the metabolic conversion and degradation of P450 eicosanoids called epoxyeicosatrienoic acids, EETs Rattus norvegicus