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Literature summary for 1.1.1.49 extracted from

  • Preuss, J.; Hedrick, M.; Sergienko, E.; Pinkerton, A.; Mangravita-Novo, A.; Smith, L.; Marx, C.; Fischer, E.; Jortzik, E.; Rahlfs, S.; Becker, K.; Bode, L.
    High-throughput screening for small-molecule inhibitors of Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase (2012), J. Biomol. Screen., 17, 738-751.
    View publication on PubMed

Application

Application Comment Organism
drug development the enzyme is a target for anti-parasite drug development Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
(4Z)-4-(3-bromobenzylidene)-1-(4-methylphenyl)pyrazolidine-3,5-dione
-
Plasmodium falciparum
(5Z)-1-(4-bromophenyl)-5-[[5-(2-nitrophenyl)furan-2-yl]methylidene]pyrimidine-2,4,6(1H,3H,5H)-trione
-
Plasmodium falciparum
(5Z)-1-(4-ethoxyphenyl)-5-[[5-(2-nitrophenyl)furan-2-yl]methylidene]pyrimidine-2,4,6(1H,3H,5H)-trione
-
Plasmodium falciparum
(5Z)-5-[[5-(2-methyl-4-nitrophenyl)furan-2-yl]methylidene]-1-(3-methylphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione reversible, non-competitive inhibition versus NADP+, mixed-type versus D-glucose 6-phosphate Plasmodium falciparum
2-[(5Z)-5-(4-hydroxy-3-methoxybenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoate
-
Plasmodium falciparum
2-[(E)-(4-nitrocyclohexa-2,4-dien-1-yl)(2-phenylhydrazinylidene)methyl]benzene-1,4-diol non-competitive inhibition versus NADP+, non-competitive or mixed-type versus D-glucose 6-phosphate Plasmodium falciparum
2-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]-5-methyl-4-(3,4,5-trimethoxybenzyl)-2,4-dihydro-3H-pyrazol-3-one irreversible, non-competitive inhibition versus NADP+, mixed-type versus D-glucose 6-phosphate Plasmodium falciparum
3-(4-hydroxyphenyl)-2-(pyridin-3-yl)quinazolin-4(3H)-one irreversible, non-competitive inhibition versus NADP+, mixed-type versus D-glucose 6-phosphate Plasmodium falciparum
3-(5-bromopyridin-2-yl)-2-(pyridin-3-yl)quinazolin-4(3H)-one irreversible, non-competitive inhibition versus NADP+, mixed-type versus D-glucose 6-phosphate Plasmodium falciparum
3-(5-[(E)-[2-(5-nitropyridin-2-yl)hydrazinylidene]methyl]furan-2-yl)benzoic acid
-
Plasmodium falciparum
4-fluoro-N-(4-hydroxynaphthalen-1-yl)benzenesulfonamide
-
Plasmodium falciparum
4-methyl-3-(propan-2-yloxy)-6H-benzo[c]chromen-6-one non-competitive inhibition versus NADP+, mixed-type versus D-glucose 6-phosphate Plasmodium falciparum
5-[[5-(4-methoxy-2-nitrophenyl)furan-2-yl]methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione reversible, competitive inhibition versus NADP+, mixed-type versus D-glucose 6-phosphate Plasmodium falciparum
additional information high-throughput screening for small-molecule inhibitors of the enzyme from Plasmodium falciparum, inhibitor evaluation, structure-activity relationship analysis, overview Plasmodium falciparum
N-(4-hydroxynaphthalen-1-yl)-2,5-dimethylbenzenesulfonamide
-
Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0086
-
NADP+ pH 7.5, temperature not specified in the publication Plasmodium falciparum
0.0145
-
D-glucose 6-phosphate pH 7.5, temperature not specified in the publication Plasmodium falciparum

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Plasmodium falciparum

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
107000
-
-
Plasmodium falciparum

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
D-glucose 6-phosphate + NADP+ Plasmodium falciparum
-
6-phospho-D-glucono-1,5-lactone + NADPH + H+
-
?
additional information Plasmodium falciparum the enzyme is a bifunctional enzyme glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase, the enzyme activity is analyzed for the reaction of glucose-6-phosphate dehydrogenase, EC 1.1.1.49, in a coupled assay with diaphorase activity, which uses NADPH to reduce resazurin to form the highly fluorescent molecule resorufin ?
-
?

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-glucose 6-phosphate + NADP+
-
Plasmodium falciparum 6-phospho-D-glucono-1,5-lactone + NADPH + H+
-
?
additional information the enzyme is a bifunctional enzyme glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase, the enzyme activity is analyzed for the reaction of glucose-6-phosphate dehydrogenase, EC 1.1.1.49, in a coupled assay with diaphorase activity, which uses NADPH to reduce resazurin to form the highly fluorescent molecule resorufin Plasmodium falciparum ?
-
?

Synonyms

Synonyms Comment Organism
glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase
-
Plasmodium falciparum
PfGluPho
-
Plasmodium falciparum

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00097
-
pH 7.5, temperature not specified in the publication Plasmodium falciparum 4-methyl-3-(propan-2-yloxy)-6H-benzo[c]chromen-6-one
0.0018
-
pH 7.5, temperature not specified in the publication Plasmodium falciparum 2-[(E)-(4-nitrocyclohexa-2,4-dien-1-yl)(2-phenylhydrazinylidene)methyl]benzene-1,4-diol
0.0039
-
pH 7.5, temperature not specified in the publication Plasmodium falciparum 4-fluoro-N-(4-hydroxynaphthalen-1-yl)benzenesulfonamide
0.0053
-
pH 7.5, temperature not specified in the publication Plasmodium falciparum N-(4-hydroxynaphthalen-1-yl)-2,5-dimethylbenzenesulfonamide

General Information

General Information Comment Organism
metabolism the bifunctional glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase enzyme catalyzes the first and second steps in the parasite's pentose phosphate pathway, cf. EC 3.1.1.31 Plasmodium falciparum