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Literature summary extracted from

  • Pawelzik, S.C.; Uda, N.R.; Spahiu, L.; Jegerschoeld, C.; Stenberg, P.; Hebert, H.; Morgenstern, R.; Jakobsson, P.J.
    Identification of key residues determining species differences in inhibitor binding of microsomal prostaglandin E synthase-1 (2010), J. Biol. Chem., 285, 29254-29261.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.3.99.3 expressed in Escherichia coli BL21Star (DE) pLysS cells Homo sapiens
5.3.99.3 expressed in Escherichia coli BL21Star (DE) pLysS cells Rattus norvegicus

Protein Variants

EC Number Protein Variants Comment Organism
5.3.99.3 T131V/L135F/A138F the mutant shows bout 4fold reduced specific activity towards prostaglandin H2 compared to the wild type enzyme and is not inhibited by 1-C-(2-chlorobenzene)-3-N-(naphthalen-1-yl)benzene-1,3-dicarboxamide Homo sapiens
5.3.99.3 V131T/F135L/F138A the mutant shows bout 4fold increased specific activity towards prostaglandin H2 compared to the wild type enzyme and is inhibited by 1-C-(2-chlorobenzene)-3-N-(naphthalen-1-yl)benzene-1,3-dicarboxamide Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 (4E)-4-[2-(3-bromophenyl)hydrazin-1-ylidene]-1-ethanethioyl-3-methyl-4,5-dihydro-1H-pyrazol-5-one
-
 Homo sapiens
5.3.99.3 (4E)-4-[2-(3-bromophenyl)hydrazin-1-ylidene]-1-ethanethioyl-3-methyl-4,5-dihydro-1H-pyrazol-5-one
-
 Rattus norvegicus
5.3.99.3 2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide selective for human over rat MPGES1 Homo sapiens
5.3.99.3 2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide inhibitor of mutant enzyme V131T/F135L/F138A, but not of the wild type enzyme Rattus norvegicus

Localization

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

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.3.99.3 Prostaglandin H2 Homo sapiens
-
 Prostaglandin E2
-
 ?
5.3.99.3 Prostaglandin H2 Rattus norvegicus
-
 Prostaglandin E2
-
 ?

Organism

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

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
5.3.99.3 0.054
-
 mutant enzyme T131V/L135F/A138F, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C Homo sapiens
5.3.99.3 0.059
-
 wild type enzyme, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C Rattus norvegicus
5.3.99.3 0.086
-
 mutant enzyme V131T/F135L/F138A, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C Rattus norvegicus
5.3.99.3 0.214
-
 wild type enzyme, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.99.3 Prostaglandin H2
-
 Homo sapiens Prostaglandin E2
-
 ?
5.3.99.3 Prostaglandin H2
-
 Rattus norvegicus Prostaglandin E2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.3.99.3 microsomal prostaglandin E synthase-1
-
 Homo sapiens
5.3.99.3 microsomal prostaglandin E synthase-1
-
 Rattus norvegicus
5.3.99.3 MPGES1
-
 Homo sapiens
5.3.99.3 MPGES1
-
 Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
5.3.99.3 glutathione
-
 Homo sapiens
5.3.99.3 glutathione
-
 Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.3 0.000058
-
 wild type enzyme, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C Homo sapiens 2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide
5.3.99.3 0.00059
-
 mutant enzyme V131T/F135L/F138A, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C Rattus norvegicus 2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide