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Literature summary for 1.13.11.31 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)

Cloned (Comment) Organism
expression of N-terminally His6-tagged enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
alpha-mangostin NSC30552, a natural product, caspase-3 pathway inhibitor, performs selective inhibition of 12-LO Homo sapiens
dysidenin
-
Homo sapiens
michellamine B NSC661755, potent but non-selective inhibitor, a natural anti-viral agent Homo sapiens
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
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
NSC172033 a synthetic compound from the NCI library Homo sapiens
NSC292213 a synthetic compound from the NCI library Homo sapiens
NSC617570 a synthetic compound from the NCI library 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 P18054
-
-

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
platelet-type 12-human lipoxygenase
-
Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.017
-
neodysidenin pH 8.0, recombinant enzyme Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00015
-
pH 8.0, recombinant enzyme Homo sapiens NSC292213
0.00019
-
pH 8.0, recombinant enzyme Homo sapiens NSC617570
0.00021
-
pH 8.0, recombinant enzyme Homo sapiens NSC172033
0.00058
-
pH 8.0, recombinant enzyme Homo sapiens alpha-mangostin
0.0049
-
pH 8.0, recombinant enzyme Homo sapiens michellamine B
0.009
-
above, pH 8.0, recombinant enzyme Homo sapiens dysidenin
0.1
-
above, pH 8.0, recombinant enzyme Homo sapiens neodysidenin