Activating Compound | Comment | Organism | Structure |
---|---|---|---|
FLAP | 5-lipoxygenase-activating protein. Inhibitor BRP-7 blocks 5-LOX co-localization with FLAP at the nuclear envelope in neutrophils | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-[2-[(2-methyl-1H-benzimidazol-1-yl)methyl]phenoxy]acetamide | a BRP-7 derivative | Homo sapiens | |
2-[2-[(2-[1-[4-(2-methylpropyl)phenyl]ethyl]-1H-benzimidazol-1-yl)methyl]phenoxy]acetamide | a BRP-7 derivative | Homo sapiens | |
BRP-7 | benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP). BRP-7 blocks 5-LOX co-localization with FLAP at the nuclear envelope in neutrophils. No complete inhibition up to 0.01 mM | Homo sapiens | |
ethyl [2-[(2-[1-[4-(2-methylpropyl)phenyl]ethyl]-1H-benzimidazol-1-yl)methyl]phenoxy]acetate | a BRP-7 derivative | Homo sapiens | |
MK886 | - |
Homo sapiens | |
additional information | immobilization of BRP-7 derivatives and pull-down assays, overview | Homo sapiens | |
zileuton | - |
Homo sapiens | |
[2-[(2-methyl-1H-benzimidazol-1-yl)methyl]phenoxy]acetyl chloride | a BRP-7 derivative | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
cytosol | - |
Homo sapiens | 5829 | - |
additional information | upon stimulation of neutrophils with A23187, cytosolic 5-LOX is translocated to the nucleus, and this is concentration-dependently inhibited by BRP-7 | Homo sapiens | - |
- |
nuclear envelope | - |
Homo sapiens | 5635 | - |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Ca2+ | required | Homo sapiens | |
Fe2+ | required | Homo sapiens |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P09917 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
neutrophil | stimulated with A23187 | Homo sapiens | - |
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 | Comment | Organism |
---|---|---|
5-lipoxygenase | - |
Homo sapiens |
5-LOX | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0011 | - |
pH 7.4, 37°C | Homo sapiens | MK886 | |
0.0048 | - |
pH 7.4, 37°C | Homo sapiens | BRP-7 |