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Literature summary for 2.7.1.82 extracted from

  • Alberge, B.; Gannoun-Zaki, L.; Bascunana, C.; Tran van Ba, C.; Vial, H.; Cerdan, R.
    Comparison of the cellular and biochemical properties of Plasmodium falciparum choline and ethanolamine kinases (2010), Biochem. J., 425, 149-158.
    View publication on PubMed

Application

Application Comment Organism
medicine ethanolamine kinase could be a target for antimalerial therapy Plasmodium falciparum 3D7

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Plasmodium falciparum
into the vector pET24b for expression in Escherichia coli BL21DE3-pRIL cells Plasmodium falciparum 3D7

Inhibitors

Inhibitors Comment Organism Structure
2-amino-1-butanol analogue of ethanolamine, selective inhibition Plasmodium falciparum
2-amino-1-butanol
-
Plasmodium falciparum 3D7
3,3'-dodecane-1,12-diylbis[5-(2-hydroxyethyl)-4-methyl-1,3-thiazol-3-ium] SAR97276 Plasmodium falciparum 3D7
hemicholinium-3
-
Plasmodium falciparum
SAR97276 bis-thiazolium compound designed as a choline analogue, affects ethanolamine kinase and choline kinase activities similarly. Inhibition is competitive and correlates with the impairment of cellular phosphatidylcholine biosynthesis Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.458
-
ethanolamine pH 8.0, 37°C Plasmodium falciparum
0.4757
-
ethanolamine
-
Plasmodium falciparum 3D7

Localization

Localization Comment Organism GeneOntology No. Textmining
cytoplasm
-
Plasmodium falciparum 3D7 5737
-
cytoplasm of Plasmodium falciparum Plasmodium falciparum 5737
-
additional information protein expression levels increase during erythrocytic development Plasmodium falciparum
-
-

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
48000
-
determined by SDS-PAGE and Western Blot analysis Plasmodium falciparum 3D7
109000
-
determined by gel filtration Plasmodium falciparum 3D7

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + ethanolamine Plasmodium falciparum 3D7
-
ADP + O-phosphoethanolamine
-
?

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q8IIB7 3D7
-
Plasmodium falciparum 3D7 Q8IIB7
-
-

Purification (Commentary)

Purification (Comment) Organism
using a HisTrap chelating and a gel filtration column Plasmodium falciparum 3D7

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.3
-
pH 8.0, 37°C Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + ethanolamine
-
Plasmodium falciparum 3D7 ADP + O-phosphoethanolamine
-
?
ATP + ethanolamine
-
Plasmodium falciparum ADP + O-phosphoethanolamine
-
?
additional information no substrate: choline Plasmodium falciparum ?
-
?

Subunits

Subunits Comment Organism
homodimer
-
Plasmodium falciparum 3D7

Synonyms

Synonyms Comment Organism
ethanolamine kinase
-
Plasmodium falciparum 3D7
PfEK
-
Plasmodium falciparum 3D7

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
activity assay Plasmodium falciparum 3D7

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
activity assay Plasmodium falciparum 3D7

Cofactor

Cofactor Comment Organism Structure
ATP
-
Plasmodium falciparum 3D7

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.73
-
3,3'-dodecane-1,12-diylbis[5-(2-hydroxyethyl)-4-methyl-1,3-thiazol-3-ium]
-
Plasmodium falciparum 3D7

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.46
-
pH 8.0, 37°C Plasmodium falciparum hemicholinium-3
0.46
-
Plasmodium falciparum-endogenous ethanolamine kinase Plasmodium falciparum 3D7 2-amino-1-butanol
0.61
-
recombinant protein Plasmodium falciparum 3D7 3,3'-dodecane-1,12-diylbis[5-(2-hydroxyethyl)-4-methyl-1,3-thiazol-3-ium]
0.79
-
pH 8.0, 37°C Plasmodium falciparum SAR97276
0.79
-
Plasmodium falciparum-endogenous ethanolamine kinase Plasmodium falciparum 3D7 3,3'-dodecane-1,12-diylbis[5-(2-hydroxyethyl)-4-methyl-1,3-thiazol-3-ium]
1.36
-
pH 8.0, 37°C Plasmodium falciparum 2-amino-1-butanol
1.36
-
recombinant protein Plasmodium falciparum 3D7 2-amino-1-butanol

Expression

Organism Comment Expression
Plasmodium falciparum 3D7 expression levels increases during erythrocytic development up