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Literature summary for 1.13.11.34 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.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.13.11.34

Inhibitors

Inhibitors Comment Organism Structure
1-(3-[5-(hydroxyureido)methyl-2-methoxyphenoxy]propyl)-3-[4-(trifluoromethoxy)phenyl]urea KM55, a multitarget ligand and dual 5-lipoxygenase (5-LO)/soluble epoxide hydrolase (sEH) inhibitor. KM55 potently inhibits both enzymes in vitro and attenuates the formation of leukotrienes in human whole blood. It significantly inhibits the LPS-induced adhesion of leukocytes to endothelial cells by blocking leukocyte activation. Compound synthesis and evaluation, overview. KM55 inhibits the formation of leukotriene B4 and 5-hydroxyeicosatrienoic acid, while the formation of 12-hydroperoxyicosatetraenoate and 15-hydroperoxyicosatetraenoate are unaffected. KM55 blocks leukocyte-endothelial cell interaction by impairing leukocyte activation, whereas endothelial cells are not affected Homo sapiens
zileuton
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
arachidonate + O2 Homo sapiens
-
 (5S,6S,7E,9E,11Z,14Z)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P09917
-
-

Source Tissue

Source Tissue Comment Organism Textmining
endothelial cell
-
 Homo sapiens
-
endothelial cell primary Homo sapiens
-
leukocyte
-
 Homo sapiens
-
THP-1 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
arachidonate + O2
-
 Homo sapiens (5S,6S,7E,9E,11Z,14Z)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
-
 ?

Synonyms

Synonyms Comment Organism
5-lipoxygenase
-
 Homo sapiens
5-LO
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0013
-
 pH 7.4, 37°C Homo sapiens 1-(3-[5-(hydroxyureido)methyl-2-methoxyphenoxy]propyl)-3-[4-(trifluoromethoxy)phenyl]urea