Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli HB101 cells | Homo sapiens |
expression Escherichia coli HB101 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(5Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(1E,3S)-3-hydroxy-5-phenylpent-1-en-1-yl]cyclopentyl]-N-ethylhept-5-enamide | bimatoprost | Homo sapiens | |
(5Z)-7-[(1R,4S,5S,6R)-6-[(1E)-oct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | ONO1370 | Homo sapiens | |
(5Z)-7-[(1R,4S,5S,6R)-6-[(1E,3S)-3-hydroxyoct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | ONO1349 | Homo sapiens | |
(5Z)-7-[(1S,4S,5S,6R)-2-methyl-6-[(1E)-oct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | ONO1373 | Homo sapiens | |
(Z)-7-[(1R,4S,5S,6R)-((E)-6-oct-1-enyl)-2-aza-bicyclo[2.2.1]hept-5-yl]-hept-5-enoic acid | inhibition of PGH2 9,11-endoperoxide reductase activity, slight inhibition of prostamide D2 11-ketoreductase and PGD2 11-ketoreductase activity | Homo sapiens | |
(Z)-7-[(1R,4S,5S,6R)-2-methyl-6-((E)-oct-1-enyl)-2-aza-bicyclo[2.2.1]hept-5-yl]-hept-5-enoic acid | inhibition of PGH2 9,11-endoperoxide reductase activity, slight inhibition of prostamide D2 11-ketoreductase and PGD2 11-ketoreductase activity, competitive, binds to the active site | Homo sapiens | |
(Z)-7-[(1R,4S,5S,6R)-6-((E)-(S)-3-hydroxy-oct-1-enyl)-2-aza-bicyclo[2.2.1]hept-5-yl]-hept-5-enoic acid | inhibition of PGH2 9,11-endoperoxide reductase activity, slight inhibition of prostamide D2 11-ketoreductase and PGD2 11-ketoreductase activity | Homo sapiens | |
bimatoprost | ethyl amide analogue of 17-phenyl-trinor PGF2alpha, inhibits all enzyme activities noncompetitively at low concentration, binds to a site different from the active site; potent inhibitor | Homo sapiens | |
ONO1349 | - |
Homo sapiens | |
ONO1370 | - |
Homo sapiens | |
ONO1373 | - |
Homo sapiens | |
Tolrestat | inhibition of all 3 enzyme activities, most effective inhibiting the PGD2 11-ketoreductase activity | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Homo sapiens | P42330 | - |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
recombinant enzyme from Escherichia coli, to homogeneity | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | substrate and product detection by liquid chromatographic-electrospray ionization-mass spectrometry | Homo sapiens | ? | - |
? | |
prostaglandin D2 + NADPH + H+ | - |
Homo sapiens | prostaglandin 9alpha,11beta-F2 + NADP+ | - |
? | |
prostaglandin D2 + NADPH + H+ | - |
Homo sapiens | prostaglandin F2alpha + NADP+ | - |
? | |
prostaglandin D2 + NADPH + H+ | - |
Homo sapiens | 9alpha,11beta-prostaglandin F2 + NADP+ | - |
? | |
prostaglandin D2 ethanolamide + NADPH | i.e. prostamide D2 | Homo sapiens | prostaglandin 9alpha,11beta-F2 ethanolamide + NADP+ | i.e. 91lpha,11beta-prostamide F2 | ? | |
prostaglandin H2 + NADPH + H+ | - |
Homo sapiens | prostaglandin F2alpha + NADP+ | - |
? | |
prostaglandin H2 + NADPH + H+ | - |
Homo sapiens | prostaglandin 9alpha,11beta-F2 + NADP+ | - |
? | |
prostamide D2 + NADPH + H+ | - |
Homo sapiens | 9alpha,11beta-prostamide F2 + NADP+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PGD2 11-ketoreductase | - |
Homo sapiens |
PGF synthase | - |
Homo sapiens |
PGH2 9,11-endoperoxide reductase | - |
Homo sapiens |
prostaglandin F synthase | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
PGD2 11-ketoreductase activity assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
6.5 | - |
PGD2 11-ketoreductase activity assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.005 | - |
recombinant enzyme, using prostaglandin D2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(1E,3S)-3-hydroxy-5-phenylpent-1-en-1-yl]cyclopentyl]-N-ethylhept-5-enamide | |
0.005 | - |
recombinant enzyme, using prostaglandin D2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | bimatoprost | |
0.006 | - |
recombinant enzyme, using prostaglandin H2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(1E,3S)-3-hydroxy-5-phenylpent-1-en-1-yl]cyclopentyl]-N-ethylhept-5-enamide | |
0.006 | - |
recombinant enzyme, using prostaglandin H2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | bimatoprost | |
0.06 | - |
recombinant enzyme, using prostaglandin H2 2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | ONO1373 | |
0.06 | - |
recombinant enzyme, using prostaglandin H2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1S,4S,5S,6R)-2-methyl-6-[(1E)-oct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | |
0.06 | - |
recombinant enzyme, using prostamide D2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(1E,3S)-3-hydroxy-5-phenylpent-1-en-1-yl]cyclopentyl]-N-ethylhept-5-enamide | |
0.06 | - |
recombinant enzyme, using prostamide D2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | bimatoprost | |
0.1 | - |
recombinant enzyme, using prostaglandin D2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | Tolrestat | |
0.13 | - |
recombinant enzyme, using prostaglandin H2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1R,4S,5S,6R)-6-[(1E,3S)-3-hydroxyoct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | |
0.13 | - |
recombinant enzyme, using prostaglandin H2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | ONO1349 | |
0.3 | - |
recombinant enzyme, using prostaglandin H2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1R,4S,5S,6R)-6-[(1E)-oct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | |
0.3 | - |
recombinant enzyme, using prostaglandin H2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | Tolrestat | |
0.3 | - |
recombinant enzyme, using prostaglandin H2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | ONO1370 | |
0.45 | - |
recombinant enzyme, using prostamide D2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | Tolrestat | |
1 | - |
IC50 about 1 mM, recombinant enzyme, using prostaglandin D2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1S,4S,5S,6R)-2-methyl-6-[(1E)-oct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | |
1 | - |
IC50 about 1 mM, recombinant enzyme, using prostaglandin D2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1R,4S,5S,6R)-6-[(1E,3S)-3-hydroxyoct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | |
1 | - |
IC50 about 1 mM, recombinant enzyme, using prostaglandin D2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1R,4S,5S,6R)-6-[(1E)-oct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | |
1 | - |
IC50 about 1 mM, recombinant enzyme, using prostamide D2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1S,4S,5S,6R)-2-methyl-6-[(1E)-oct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | |
1 | - |
IC50 about 1 mM, recombinant enzyme, using prostamide D2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1R,4S,5S,6R)-6-[(1E,3S)-3-hydroxyoct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | |
1 | - |
IC50 about 1 mM, recombinant enzyme, using prostamide D2 as substrate, in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | (5Z)-7-[(1R,4S,5S,6R)-6-[(1E)-oct-1-en-1-yl]-2-azabicyclo[2.2.1]hept-5-yl]hept-5-enoic acid | |
1 | - |
recombinant enzyme, using prostaglandin D2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | ONO1373 | |
1 | - |
recombinant enzyme, using prostaglandin D2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | ONO1349 | |
1 | - |
recombinant enzyme, using prostaglandin D2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | ONO1370 | |
1 | - |
recombinant enzyme, using prostamide D2 2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | ONO1373 | |
1 | - |
recombinant enzyme, using prostamide D2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | ONO1349 | |
1 | - |
recombinant enzyme, using prostamide D2 as substrate,in 0.1 M potassium phosphate buffer, pH 6.5, at 37°C | Homo sapiens | ONO1370 |