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Literature summary for 3.3.2.10 extracted from

  • Meirer, K.; Glatzel, D.; Kretschmer, S.; Wittmann, S.K.; Hartmann, M.; Bloecher, R.; Angioni, C.; Geisslinger, G.; Steinhilber, D.; Hofmann, B.; Fuerst, R.; Proschak, E.
    Design, synthesis and cellular characterization of a dual inhibitor of 5-lipoxygenase and soluble epoxide hydrolase (2016), Molecules, 22, 45-54 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
1-(3-(5-(hydroxyureido)methyl-2-methoxyphenoxy)propyl)-3-[4-(trifluoromethoxy)phenyl]urea i.e. KM55, a dual inhibitor of 5-lipoxygenase (5-LO) and soluble epoxide hydrolase (sEH), synthesis and evaluation, overview. Applied to leukocytes, it strongly inhibits the lipopolysaccharide (LPS)-induced adhesion of the leukocytes to endothelial cells. KM55 is a designed multi-target ligand which inhibits the enzymatic activity of 5-LO and sEH Homo sapiens
N-cyclohexyl-N'-(4-iodophenyl)urea CIU Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
epoxyeicosatrienoic acid + H2O Homo sapiens
-
dihydroxyeicosatrienoic acid
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P34913
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3-phenyl-cyano-(6-methoxy-2-naphthalenyl)methylester-2-oxirane-acetic acid + H2O the non-fluorescent substrate can be hydrolyzed by enzyme sEH to the fluorescent 6-methoxynaphtaldehyde Homo sapiens 6-methoxynaphtaldehyde + ?
-
?
epoxyeicosatrienoic acid + H2O
-
Homo sapiens dihydroxyeicosatrienoic acid
-
?

Synonyms

Synonyms Comment Organism
SEH
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000029
-
recombinant enzyme, pH 7.0, 22°C Homo sapiens 1-(3-(5-(hydroxyureido)methyl-2-methoxyphenoxy)propyl)-3-[4-(trifluoromethoxy)phenyl]urea
0.00014
-
recombinant enzyme, pH 7.0, 22°C Homo sapiens N-cyclohexyl-N'-(4-iodophenyl)urea