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Literature summary for 1.3.1.48 extracted from

  • Piao, Y.; Wu, Y.; Seo, S.; Lim, S.; Cho, H.
    Wound healing effects of new 15-hydroxyprostaglandin dehydrogenase inhibitors (2014), Prostaglandins Leukot. Essent. Fatty Acids, 91, 325-332 .
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression as GST-tagged enzyme in Escherichiacoli strain BL-21LysS Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5-(2-chloro-3-((4-methylcyclohexyl)methoxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-((5-oxo-5,6,7,8-tetrahydronaphthalen-1-yl)oxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(1-cyclopropylethoxy)benzylidene)-1,3- thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(2-(4-methyl-1,3-thiazolidin-5-yl)ethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(2-(cyclohexyloxy)ethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(2-(propan-2-yloxy)ethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(2-(pyridin-2-yl)ethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(2-cyclohexylethoxy)benzylidene)thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(2-cyclopentylethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(3-cyclohexylpropoxy)benzylidene)thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(3-nitrophenoxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(3-phenylpropoxy)benzylidene)thiazolidine-2,4-dione the compound significantly increases the level of PGE2 in skin defects Homo sapiens
5-(2-chloro-3-(4-cyclohexylbutoxy)benzylidene)thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(4-nitrobenzyloxy)benzylidene)thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(4-phenylbutoxy)benzylidene)thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(cyclobutylmethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(cyclohexylmethoxy)benzylidene)thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(cyclohexyloxy)benzylidene)thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(cyclopentylmethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-(cyclopentyloxy)benzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
5-(2-chloro-3-phenethoxybenzylidene)thiazolidine-2,4-dione
-
Homo sapiens
5-(3-(benzyloxy)-2-chlorobenzylidene)thiazolidine-2,4-dione
-
Homo sapiens
5-(3-(bicyclo[2.2.1]hept-2-ylmethoxy)-2-chlorobenzylidene)-1,3-thiazolidine-2,4-dione
-
Homo sapiens
ciglitazone
-
Homo sapiens
additional information thiazolidinediones as enzyme inhibitors. No inhibition by 5-(2-chloro-3-(1-cyclopropylethoxy)benzylidene)-1,3-thiazolidine-2,4-dione Homo sapiens
thiazolidinedione
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
prostaglandin E2 + NADP+ Homo sapiens
-
15-ketoprostaglandin E2 + NADPH + H+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
Homo sapiens
-
HaCaT cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
prostaglandin E2 + NADP+
-
Homo sapiens 15-ketoprostaglandin E2 + NADPH + H+
-
?

Synonyms

Synonyms Comment Organism
15-hydroxyprostaglandin dehydrogenase
-
Homo sapiens
15-PGDH
-
Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00002
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(cyclopentylmethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.000029
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(2-cyclohexylethoxy)benzylidene)thiazolidine-2,4-dione
0.000045
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(3-phenylpropoxy)benzylidene)thiazolidine-2,4-dione
0.000054
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(4-phenylbutoxy)benzylidene)thiazolidine-2,4-dione
0.000058
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(cyclohexylmethoxy)benzylidene)thiazolidine-2,4-dione
0.000059
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(3-cyclohexylpropoxy)benzylidene)thiazolidine-2,4-dione
0.000095
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(4-cyclohexylbutoxy)benzylidene)thiazolidine-2,4-dione
0.000122
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-phenethoxybenzylidene)thiazolidine-2,4-dione
0.00013
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-((5-oxo-5,6,7,8-tetrahydronaphthalen-1-yl)oxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.00014
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-((4-methylcyclohexyl)methoxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.00014
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(3-nitrophenoxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.00015
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(2-cyclopentylethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.00017
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(2-(propan-2-yloxy)ethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.000212
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(cyclohexyloxy)benzylidene)thiazolidine-2,4-dione
0.00023
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(2-(cyclohexyloxy)ethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.000257
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(3-(benzyloxy)-2-chlorobenzylidene)thiazolidine-2,4-dione
0.00036
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(cyclobutylmethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.00109
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(2-(4-methyl-1,3-thiazolidin-5-yl)ethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.00258
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(cyclopentyloxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.00862
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(3-(bicyclo[2.2.1]hept-2-ylmethoxy)-2-chlorobenzylidene)-1,3-thiazolidine-2,4-dione
0.0103
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(2-(pyridin-2-yl)ethoxy)benzylidene)-1,3-thiazolidine-2,4-dione
0.0117
-
pH 75, 37°C, recombinant GST-tagged enzyme Homo sapiens 5-(2-chloro-3-(4-nitrobenzyloxy)benzylidene)thiazolidine-2,4-dione

General Information

General Information Comment Organism
physiological function prostaglandin E2, PGE2, has a short half-life in vivo because is rapidly oxidized to 15-ketoprostaglandins by the cytosolic enzyme 15-PGDH. PGE2 acts through EP2 and EP4 receptors to mediate regeneration and hematopoietic stem cell development via the Wnt signaling pathway. Wnt activation in stem cells requires PGE2, and the PGE2/Wnt interaction is a master regulator of vertebrate regeneration and recovery. PGE2 regulates vertebrate hematopoietic stem cell induction and engraftment Homo sapiens