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Literature summary 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.
    View publication on PubMed

Application

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.3.2.6 (R)-2-(4-benzylphenoxymethyl)pyrrolidine
-
 Homo sapiens
3.3.2.6 (R)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidine
-
 Homo sapiens
3.3.2.6 4-((R)-2-(4-(4-chlorophenoxy)phenoxymethyl)pyrrolidin-1-yl)-l-butyric acid
-
 Homo sapiens
3.3.2.6 4-((S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl)-butyric acid
-
 Homo sapiens
3.3.2.6 4-[(2S)-2-([4-(4-chlorophenoxy)phenoxy]methyl)-1-pyrrolidinyl]butanoic acid i.e. DG-051 Homo sapiens
3.3.2.6 additional information inhibitor structure-function analysis, overview Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.3.2.6 microsome
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
3.3.2.6 Homo sapiens P09960
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.3.2.6 heart
-
 Homo sapiens
-
3.3.2.6 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
3.3.2.6 leukotriene A4 hydrolase
-
 Homo sapiens
3.3.2.6 LTA4H
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.3.2.6 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.3.2.6 8
-
 assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.3.2.6 0.00003
-
-
 Homo sapiens (R)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidine
3.3.2.6 0.000047
-
-
 Homo sapiens 4-((S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl)-butyric acid
3.3.2.6 0.000087
-
-
 Homo sapiens (R)-2-(4-benzylphenoxymethyl)pyrrolidine

General Information

EC Number General Information Comment Organism
3.3.2.6 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