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Literature summary extracted from

  • Deschamps, J.D.; Gautschi, J.T.; Whitman, S.; Johnson, T.A.; Gassner, N.C.; Crews, P.; Holman, T.R.
    Discovery of platelet-type 12-human lipoxygenase selective inhibitors by high-throughput screening of structurally diverse libraries (2007), Bioorg. Med. Chem., 15, 6900-6908.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.13.11.31 expression of N-terminally His6-tagged enzyme Homo sapiens
1.13.11.33 expression of isozyme 15-hLO-2 in Spodoptera frugiperda Sf9 cells using the baculovirus transfection system, expression of N-terminally His6-tagged 15-hLO-1 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.13.11.31 alpha-mangostin NSC30552, a natural product, caspase-3 pathway inhibitor, performs selective inhibition of 12-LO Homo sapiens
1.13.11.31 dysidenin
-
 Homo sapiens
1.13.11.31 michellamine B NSC661755, potent but non-selective inhibitor, a natural anti-viral agent Homo sapiens
1.13.11.31 additional information development of an assay method for high throughput screening of libraries for platelet-type 12-hLO selective inhibitors, four organo-mercurial compounds with NCI library IDs NSC20410, NSC268879, NSC321237, and NSC321239, are also found to be selectively inhibitory, but not pursued further due to their potentially toxic side effects, overview Homo sapiens
1.13.11.31 neodysidenin natural product from marine sponge Dysidea herbacea from Papua New Guinea, extraction and purification, overview, steady-state inhibition kinetics, competitive mode of inhibition, selective for 12-LO Homo sapiens
1.13.11.31 NSC172033 a synthetic compound from the NCI library Homo sapiens
1.13.11.31 NSC292213 a synthetic compound from the NCI library Homo sapiens
1.13.11.31 NSC617570 a synthetic compound from the NCI library Homo sapiens
1.13.11.33 alpha-mangostin NSC30552, a natural product, caspase-3 pathway inhibitor, performs selective inhibition of 12-LO Homo sapiens
1.13.11.33 dysidenin
-
 Homo sapiens
1.13.11.33 michellamine B NSC661755, potent but non-selective inhibitor, a natural anti-viral agent Homo sapiens
1.13.11.33 additional information development of an assay method for high throughput screening of libraries for platelet-type 12-hLO selective inhibitors, four organo-mercurial compounds with NCI library IDs NSC20410, NSC268879, NSC321237, and NSC321239, are also found to be selectively inhibitory, but not pursued further due to their potentially toxic side effects, overview Homo sapiens
1.13.11.33 neodysidenin natural product from marine sponge Dysidea herbacea from Papua New Guinea, extraction and purification, overview, steady-state inhibition kinetics, competitive mode of inhibition, selective for 12-LO Homo sapiens
1.13.11.33 NSC172033 a synthetic compound from the NCI library Homo sapiens
1.13.11.33 NSC292213 a synthetic compound from the NCI library Homo sapiens
1.13.11.33 NSC617570 a synthetic compound from the NCI library Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.13.11.31 arachidonate + O2 Homo sapiens
-
 (5Z,8Z,10E,14Z)-(12S)-12-hydroperoxyeicosa-5,8,10,14-tetraenoate
-
 ?
1.13.11.33 arachidonate + O2 Homo sapiens
-
 (5Z,8Z,11Z,13E)-(15S)-15-hydroperoxyeicosa-5,8,11,13-tetraenoate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.13.11.31 Homo sapiens P18054
-
-
1.13.11.33 Homo sapiens
-
 isozymes 15-hLO-1 and 15-hLO-2
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.13.11.31 arachidonate + O2
-
 Homo sapiens (5Z,8Z,10E,14Z)-(12S)-12-hydroperoxyeicosa-5,8,10,14-tetraenoate
-
 ?
1.13.11.33 arachidonate + O2
-
 Homo sapiens (5Z,8Z,11Z,13E)-(15S)-15-hydroperoxyeicosa-5,8,11,13-tetraenoate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.13.11.31 platelet-type 12-human lipoxygenase
-
 Homo sapiens
1.13.11.33 human prostate epithelial 15-lipoxygenase-2
-
 Homo sapiens
1.13.11.33 reticulocyte-type 15-human lipoxygenase
-
 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.13.11.31 8
-
 assay at Homo sapiens
1.13.11.33 7.5
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.13.11.31 0.017
-
 neodysidenin pH 8.0, recombinant enzyme Homo sapiens
1.13.11.33 0.008
-
 dysidenin above, pH 7.5, recombinant isozyme 15-hLO-1 Homo sapiens
1.13.11.33 0.5
-
 neodysidenin above, pH 7.5, recombinant isozyme 15-hLO-1 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.13.11.31 0.00015
-
 pH 8.0, recombinant enzyme Homo sapiens NSC292213
1.13.11.31 0.00019
-
 pH 8.0, recombinant enzyme Homo sapiens NSC617570
1.13.11.31 0.00021
-
 pH 8.0, recombinant enzyme Homo sapiens NSC172033
1.13.11.31 0.00058
-
 pH 8.0, recombinant enzyme Homo sapiens alpha-mangostin
1.13.11.31 0.0049
-
 pH 8.0, recombinant enzyme Homo sapiens michellamine B
1.13.11.31 0.009
-
 above, pH 8.0, recombinant enzyme Homo sapiens dysidenin
1.13.11.31 0.1
-
 above, pH 8.0, recombinant enzyme Homo sapiens neodysidenin
1.13.11.33 0.0031
-
 pH 7.5, recombinant isozyme 15-hLO-1 Homo sapiens alpha-mangostin
1.13.11.33 0.0076
-
 pH 7.5, recombinant isozyme 15-hLO-1 Homo sapiens michellamine B
1.13.11.33 0.0094
-
 pH 7.5, recombinant isozyme 15-hLO-1 Homo sapiens NSC172033
1.13.11.33 0.025
-
 pH 7.5, recombinant isozyme 15-hLO-1 Homo sapiens NSC292213
1.13.11.33 0.05
-
 above, pH 7.5, recombinant isozyme 15-hLO-2 Homo sapiens alpha-mangostin
1.13.11.33 0.05
-
 above, pH 7.5, recombinant isozyme 15-hLO-2 Homo sapiens NSC292213
1.13.11.33 0.05
-
 above, pH 7.5, recombinant isozyme 15-hLO-2 Homo sapiens michellamine B
1.13.11.33 0.05
-
 above, pH 7.5, recombinant isozyme 15-hLO-2 Homo sapiens NSC172033
1.13.11.33 0.05
-
 above, pH 7.5, recombinant isozyme 15-hLO-2 Homo sapiens NSC617570
1.13.11.33 0.5
-
 above, pH 7.5, recombinant isozyme 15-hLO-1 Homo sapiens neodysidenin
1.13.11.33 0.5
-
 above, pH 7.5, recombinant isozyme 15-hLO-1 Homo sapiens NSC617570