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Literature summary for 5.3.99.2 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)

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens O60760
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-IMAC chromatography Homo sapiens

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
hematopoietic prostaglandin D2 synthase
-
Homo sapiens
HPGDS
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
glutathione
-
Homo sapiens

Ki Value [mM]

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

IC50 Value

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