Literature summary for 3.3.2.6 extracted from

Sandanayaka, V.; Mamat, B.; Mishra, R.K.; Winger, J.; Krohn, M.; Zhou, L.M.; Keyvan, M.; Enache, L.; Sullins, D.; Onua, E.; Zhang, J.; Halldorsdottir, G.; Sigthorsdottir, H.; Thorlaksdottir, A.; Sigthorsson, G.; Thorsteinnsdottir, M.; Davies, D.R.; Stewart, L.J.; Zembower, D.E.; Andresson, T.; Kise, K.i.s.e.l.
Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis (2010), J. Med. Chem., 53, 573-585.

Application

Application	Comment	Organism
pharmacology	leukotriene 4 hydrolase is a key target for the treatment of cardiovascular disease	Homo sapiens

Inhibitors	Comment	Organism
(R)-2-(4-benzylphenoxymethyl)pyrrolidine	-	Homo sapiens
(R)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidine	-	Homo sapiens
4-((R)-2-(4-(4-chlorophenoxy)phenoxymethyl)pyrrolidin-1-yl)-l-butyric acid	-	Homo sapiens
4-((S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl)-butyric acid	-	Homo sapiens
4-[(2S)-2-([4-(4-chlorophenoxy)phenoxy]methyl)-1-pyrrolidinyl]butanoic acid	i.e. DG-051	Homo sapiens
additional information	inhibitor structure-function analysis, overview	Homo sapiens

Localization	Comment	Organism	GeneOntology No.	Textmining
microsome	-	Homo sapiens	-	-

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
leukotriene A4 + H2O	Homo sapiens	-	leukotriene B4	-	?

Organism	UniProt	Comment	Textmining
Homo sapiens	P09960	-	-

Source Tissue	Comment	Organism	Textmining
heart	-	Homo sapiens	-
liver	-	Homo sapiens	-

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
leukotriene A4 + H2O	-	Homo sapiens	leukotriene B4	-	?
leukotriene A4 + H2O	LTA4	Homo sapiens	leukotriene B4	LTB4	?

Synonyms	Comment	Organism
leukotriene A4 hydrolase	-	Homo sapiens
LTA4H	-	Homo sapiens

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	assay at	Homo sapiens

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

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.00003	-	-	Homo sapiens	(R)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidine
0.000047	-	-	Homo sapiens	4-((S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl)-butyric acid
0.000087	-	-	Homo sapiens	(R)-2-(4-benzylphenoxymethyl)pyrrolidine

General Information	Comment	Organism
metabolism	LTA4H is a key enzyme in the leukotriene pathway, which catalyzes the final and rate-determining step in the synthesis of LTB4	Homo sapiens