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Literature summary for 1.13.11.31 extracted from

  • Vasquez-Martinez, Y.; Ohri, R.V.; Kenyon, V.; Holman, T.R.; Sepulveda-Boza, S.
    Structure-activity relationship studies of flavonoids as potent inhibitors of human platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2 (2007), Bioorg. Med. Chem., 15, 7408-7425.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.13.11.31

Cloned(Commentary)

Cloned (Comment) Organism
expression of His-tagged enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-alkyl benzopyran-4-ones weak inhibition Homo sapiens
2-alkyl-6-hydroxy-4-H-benzopyran-4-one weak inhibition Homo sapiens
3'-chloro-7,8-dihydroxyisoflavone
-
 Homo sapiens
4',6,7-trihydroxyisoflavan
-
 Homo sapiens
4',6,7-trihydroxyisoflavanone
-
 Homo sapiens
4',6,7-trihydroxyisoflavone
-
 Homo sapiens
4'-chloro-7,8-dihydroxyisoflavone
-
 Homo sapiens
6,7-dihydroxy-3',4'-methylenedioxyisoflavan
-
 Homo sapiens
6,7-dihydroxy-3',4'-methylenedioxyisoflavone
-
 Homo sapiens
6,7-dihydroxy-3'-methylisoflavan
-
 Homo sapiens
6,7-dihydroxy-3'-methylisoflavanone
-
 Homo sapiens
6,7-dihydroxy-4'-methoxyisoflavan
-
 Homo sapiens
6,7-dihydroxy-4'-methoxyisoflavanone
-
 Homo sapiens
6,7-dihydroxy-4'-methoxyisoflavone
-
 Homo sapiens
6,7-dihydroxy-4'-nitroisoflavone
-
 Homo sapiens
7,8-dihydroxy-3',4'-dimethoxyisoflavan
-
 Homo sapiens
7,8-dihydroxy-3'-methylisoflavone
-
 Homo sapiens
7,8-dihydroxy-3'-trifluoromethylisoflavone
-
 Homo sapiens
7,8-dihydroxy-4'-methoxyisoflavan
-
 Homo sapiens
7,8-dihydroxy-4'-methylisoflavan
-
 Homo sapiens
7,8-dihydroxy-4'-methylisoflavone
-
 Homo sapiens
7,8-dihydroxyisoflavone
-
 Homo sapiens
7-hydroxy-H-benzopyran-4-one derivatives weak inhibition Homo sapiens
H-benzopyran-4-one derivatives weak inhibition Homo sapiens
additional information comparison of structural requirements for flavonoid inhibitory potency and selectivity against platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2, the two latter belong to EC 1.13.11.33, overview, catechols are essential for high potency, isoflavones and isoflavanones tend to select against 12-hLO, isoflavans tend to select against isozyme 15-hLO-1, but few flavonoids target isozyme 15-hLO-2, molecular modeling analysis, overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
arachidonate + O2 Homo sapiens
-
 (5Z,8Z,10E,14Z)-(12S)-12-hydroperoxyeicosa-5,8,10,14-tetraenoate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isozyme 12-hLO
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged enzyme Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood platelet isozyme 12-hLO Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
arachidonate + O2
-
 Homo sapiens (5Z,8Z,10E,14Z)-(12S)-12-hydroperoxyeicosa-5,8,10,14-tetraenoate
-
 ?

Synonyms

Synonyms Comment Organism
12-hLO
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00048
-
 pH 7.5, 22°C Homo sapiens 4'-chloro-7,8-dihydroxyisoflavone
0.00062
-
 pH 7.5, 22°C Homo sapiens 7,8-dihydroxy-3'-trifluoromethylisoflavone
0.00078
-
 pH 7.5, 22°C Homo sapiens 3'-chloro-7,8-dihydroxyisoflavone
0.0016
-
 pH 7.5, 22°C Homo sapiens 6,7-dihydroxy-4'-methoxyisoflavanone
0.0016
-
 pH 7.5, 22°C Homo sapiens 7,8-dihydroxy-4'-methylisoflavone
0.0036
-
 pH 7.5, 22°C Homo sapiens 7,8-dihydroxy-3'-methylisoflavone
0.0038
-
 pH 7.5, 22°C Homo sapiens 4',6,7-trihydroxyisoflavanone
0.0058
-
 pH 7.5, 22°C Homo sapiens 6,7-dihydroxy-4'-nitroisoflavone
0.0064
-
 pH 7.5, 22°C Homo sapiens 7,8-dihydroxyisoflavone
0.0076
-
 pH 7.5, 22°C Homo sapiens 6,7-dihydroxy-4'-methoxyisoflavan
0.0087
-
 pH 7.5, 22°C Homo sapiens 4',6,7-trihydroxyisoflavone
0.011
-
 pH 7.5, 22°C Homo sapiens 6,7-dihydroxy-3',4'-methylenedioxyisoflavan
0.014
-
 pH 7.5, 22°C Homo sapiens 6,7-dihydroxy-3'-methylisoflavanone
0.015
-
 pH 7.5, 22°C Homo sapiens 6,7-dihydroxy-3'-methylisoflavan
0.017
-
 pH 7.5, 22°C Homo sapiens 4',6,7-trihydroxyisoflavan
0.026
-
 pH 7.5, 22°C Homo sapiens 7,8-dihydroxy-4'-methoxyisoflavan
0.07
-
 pH 7.5, 22°C Homo sapiens 7,8-dihydroxy-4'-methylisoflavan
0.1
-
 above, pH 7.5, 22°C Homo sapiens 7,8-dihydroxy-3',4'-dimethoxyisoflavan
0.1
-
 above, pH 7.5, 22°C Homo sapiens 6,7-dihydroxy-4'-methoxyisoflavone
0.1
-
 above, pH 7.5, 22°C Homo sapiens 6,7-dihydroxy-3',4'-methylenedioxyisoflavone