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Literature summary extracted from

  • Koeberle, A.; Siemoneit, U.; Buehring, U.; Northoff, H.; Laufer, S.; Albrecht, W.; Werz, O.
    Licofelone suppresses prostaglandin E2 formation by interference with the inducible microsomal prostaglandin E2 synthase-1 (2008), J. Pharmacol. Exp. Ther., 326, 975-982.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
5.3.99.3 interleukin-1beta
-
 Homo sapiens

Application

EC Number Application Comment Organism
5.3.99.3 medicine licofelone suppresses inflammatory PGE2 formation preferentially by inhibiting mPGES-1 at concentrations that do not affect COX-2 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl] acetic acid licofelone, ML3000 Homo sapiens
5.3.99.3 3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2-dimethylpropanoic acid MK-886 Homo sapiens

Localization

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

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.3.99.3 (5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate Homo sapiens
-
 (5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.3 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
5.3.99.3 microsomal membranes are prepared Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.3.99.3 A-549 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.99.3 (5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
 Homo sapiens (5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.3.99.3 microsomal PGE2 synthase
-
 Homo sapiens
5.3.99.3 microsomal prostaglandin E2 synthase-1
-
 Homo sapiens
5.3.99.3 mPGES-1
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
5.3.99.3 4
-
 microsomal membranes are incubated with PGH2, enzyme activity assay Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
5.3.99.3 7.4
-
 microsomal membranes are incubated with PGH2, enzyme activity assay Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.3 0.002
-
-
 Homo sapiens 3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2-dimethylpropanoic acid
5.3.99.3 0.006
-
-
 Homo sapiens 2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl] acetic acid