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Literature summary extracted from

  • Mazari, A.M.; Hegazy, U.M.; Mannervik, B.
    Identification of new inhibitors for human hematopoietic prostaglandin D2 synthase among FDA-approved drugs and other compounds (2015), Chem. Biol. Interact., 229, 91-99 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.3.99.2 expressed in Escherichia coli XL-1 Blue cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.2 anthralin i.e. 1,8-dihydroxyanthracen-9(10H)-one Homo sapiens
5.3.99.2 bithionate sodium
-
Homo sapiens
5.3.99.2 bromocriptine mesylate
-
Homo sapiens
5.3.99.2 candesartan cilextil
-
Homo sapiens
5.3.99.2 chlorophyllide copper complex sodium salt linear competitive inhibitor Homo sapiens
5.3.99.2 deoxycorticosterone acetate
-
Homo sapiens
5.3.99.2 epirubicin hydrochloride
-
Homo sapiens
5.3.99.2 erythrosine sodium i.e. disodium 2-(2,4,5,7-tetraiodo-6-oxido-3-oxo-3H-xanthen-9-yl)benzoate Homo sapiens
5.3.99.2 Ethacrynic acid i.e. [2,3-dichloro-4-(2-methylidenebutanoyl)phenoxy]acetic acid Homo sapiens
5.3.99.2 fluorescein
-
Homo sapiens
5.3.99.2 Hexachlorophene
-
Homo sapiens
5.3.99.2 iopanic acid linear competitive inhibitor, i.e. 2-[(3-amino-2,4,6-triiodophenyl)methyl]butanoic acid Homo sapiens
5.3.99.2 Ketoprofen i.e. [3-(3-hydroxybut-3-en-2-yl)phenyl](phenyl)methanone Homo sapiens
5.3.99.2 merbromin
-
Homo sapiens
5.3.99.2 montelukast sodium
-
Homo sapiens
5.3.99.2 nisoldipine
-
Homo sapiens
5.3.99.2 pararosaniline pamoate
-
Homo sapiens
5.3.99.2 pyrvinium pamoate
-
Homo sapiens
5.3.99.2 sanguinarine sulfate linear competitive inhibitor Homo sapiens
5.3.99.2 sennoside A
-
Homo sapiens
5.3.99.2 suramin
-
Homo sapiens
5.3.99.2 Tannic acid nonlinear competitive inhibitor Homo sapiens
5.3.99.2 tranilast i.e. 2-{[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino}benzoic acid Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.3.99.2 Prostaglandin H2 Homo sapiens
-
Prostaglandin D2
-
?

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.2 Homo sapiens O60760
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
5.3.99.2 Ni-IMAC chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.99.2 1-chloro-2,4-dinitrobenzene + glutathione
-
Homo sapiens ?
-
?
5.3.99.2 1-fluoro-2,4-dinitrobenzene + glutathione
-
Homo sapiens ?
-
?
5.3.99.2 allyl isothiocyanate + glutathione
-
Homo sapiens ?
-
?
5.3.99.2 benzyl isothiocyanate + glutathione
-
Homo sapiens ?
-
?
5.3.99.2 cyclohexyl isothiocyanate + glutathione
-
Homo sapiens ?
-
?
5.3.99.2 phenethyl isothiocyanate + glutathione
-
Homo sapiens ?
-
?
5.3.99.2 propyl isothiocyanate + glutathione
-
Homo sapiens ?
-
?
5.3.99.2 Prostaglandin H2
-
Homo sapiens Prostaglandin D2
-
?

Synonyms

EC Number Synonyms Comment Organism
5.3.99.2 hematopoietic prostaglandin D2 synthase
-
Homo sapiens
5.3.99.2 HPGDS
-
Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
5.3.99.2 glutathione
-
Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
5.3.99.2 0.0001
-
suramin at pH 6.5 and 30°C Homo sapiens
5.3.99.2 0.0002
-
Tannic acid at pH 6.5 and 30°C Homo sapiens
5.3.99.2 0.001
-
sanguinarine sulfate at pH 6.5 and 30°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.2 0.0002
-
at pH 6.5 and 30°C Homo sapiens erythrosine sodium
5.3.99.2 0.0003
-
at pH 6.5 and 30°C Homo sapiens suramin
5.3.99.2 0.0004
-
at pH 6.5 and 30°C Homo sapiens Tannic acid
5.3.99.2 0.0006
-
at pH 6.5 and 30°C Homo sapiens sanguinarine sulfate
5.3.99.2 0.0017
-
at pH 6.5 and 30°C Homo sapiens chlorophyllide copper complex sodium salt
5.3.99.2 0.0018
-
at pH 6.5 and 30°C Homo sapiens iopanic acid
5.3.99.2 0.002
-
at pH 6.5 and 30°C Homo sapiens montelukast sodium
5.3.99.2 0.0033
-
at pH 6.5 and 30°C Homo sapiens merbromin
5.3.99.2 0.0055
-
at pH 6.5 and 30°C Homo sapiens candesartan cilextil
5.3.99.2 0.0084
-
at pH 6.5 and 30°C Homo sapiens epirubicin hydrochloride
5.3.99.2 0.0086
-
at pH 6.5 and 30°C Homo sapiens deoxycorticosterone acetate
5.3.99.2 0.0089
-
at pH 6.5 and 30°C Homo sapiens Hexachlorophene
5.3.99.2 0.012
-
at pH 6.5 and 30°C Homo sapiens bithionate sodium
5.3.99.2 0.0132
-
at pH 6.5 and 30°C Homo sapiens bromocriptine mesylate
5.3.99.2 0.0134
-
at pH 6.5 and 30°C Homo sapiens fluorescein
5.3.99.2 0.0137
-
at pH 6.5 and 30°C Homo sapiens tranilast
5.3.99.2 0.0172
-
at pH 6.5 and 30°C Homo sapiens pyrvinium pamoate
5.3.99.2 0.0203
-
at pH 6.5 and 30°C Homo sapiens Ketoprofen
5.3.99.2 0.0208
-
at pH 6.5 and 30°C Homo sapiens pararosaniline pamoate
5.3.99.2 0.0237
-
at pH 6.5 and 30°C Homo sapiens anthralin
5.3.99.2 0.029
-
at pH 6.5 and 30°C Homo sapiens nisoldipine
5.3.99.2 0.0393
-
at pH 6.5 and 30°C Homo sapiens sennoside A
5.3.99.2 0.044
-
at pH 6.5 and 30°C Homo sapiens Ethacrynic acid