Literature summary for 1.13.11.34 extracted from

Pergola, C.; Gerstmeier, J.; Moench, B.; Caliskan, B.; Luderer, S.; Weinigel, C.; Barz, D.; Maczewsky, J.; Pace, S.; Rossi, A.; Sautebin, L.; Banoglu, E.; Werz, O.
The novel benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP) (2014), Br. J. Pharmacol., 171, 3051-3064 .

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Activating Compound

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

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

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

Metals/Ions	Comment	Organism	Structure
Ca2+	required	Homo sapiens
Fe2+	required	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
neutrophil	stimulated with A23187	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-LOX	-	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
0.0011	-	pH 7.4, 37°C	Homo sapiens	MK886
0.0048	-	pH 7.4, 37°C	Homo sapiens	BRP-7

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Release 2023.1 (January 2023)