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Literature summary for 5.3.99.3 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
Search for more literature for 5.3.99.3

Cloned(Commentary)

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

Protein Variants

Protein Variants Comment Organism
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
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

Inhibitors Comment Organism Structure
(4E)-4-[2-(3-bromophenyl)hydrazin-1-ylidene]-1-ethanethioyl-3-methyl-4,5-dihydro-1H-pyrazol-5-one
-
 Homo sapiens
(4E)-4-[2-(3-bromophenyl)hydrazin-1-ylidene]-1-ethanethioyl-3-methyl-4,5-dihydro-1H-pyrazol-5-one
-
 Rattus norvegicus
2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide selective for human over rat MPGES1 Homo sapiens
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

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
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
0.059
-
 wild type enzyme, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C Rattus norvegicus
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
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)

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
glutathione
-
 Homo sapiens
glutathione
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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