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Literature summary for 1.1.1.267 extracted from

  • Giessmann, D.; Heidler, P.; Haemers, T.; Van Calenbergh, S.; Reichenberg, A.; Jomaa, H.; Weidemeyer, C.; Sanderbrand, S.; Wiesner, J.; Link, A.
    Towards new antimalarial drugs: synthesis of non-hydrolyzable phosphate mimics as feed for a predictive QSAR study on 1-deoxy-D-xylulose-5-phosphate reductoisomerase inhibitors (2008), Chem. Biodivers., 5, 643-656.
    View publication on PubMed

Application

Application Comment Organism
drug development Escherichia coli Dxr represents a valuable model enzyme for the screening for new antimalarial compounds, since work with the Plasmodium falciparum Dxr is associated with considerably high effort due to the instability of this enzyme and the low yield of the available recombinant expression system, no major differences in the IC50 between Escherichia coli Dxr and Plasmodium falciparum Dxr Escherichia coli
drug development Escherichia coli Dxr represents a valuable model enzyme for the screening for new antimalarial compounds, since work with the Plasmodium falciparum Dxr is associated with considerably high effort due to the instability of this enzyme and the low yield of the available recombinant expression system, no major differences in the IC50 between Escherichia coli Dxr and Plasmodium falciparum Dxr Plasmodium falciparum

Cloned(Commentary)

Cloned (Comment) Organism
dxr gene amplified and inserted into the pQE9 expression vector resulting in a protein with an amino-terminal His6-tag Escherichia coli
into the pQE31 expression vector resulting in an amino-terminal His6 fusion Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
(3S,4R)-3,4-dihydroxy-4-methyl-5-oxohexylphosphonic acid
-
Escherichia coli
3-(hydroxy([(2-phenylbutanoyl)amino]acetyl)amino)propylphosphonic acid
-
Escherichia coli
3-(hydroxy([(2-phenylbutanoyl)amino]acetyl)amino)propylphosphonic acid
-
Plasmodium falciparum
3-(hydroxy([(3-methylbutanoyl)amino]acetyl)amino)propylphosphonic acid
-
Escherichia coli
3-(hydroxy([(3-methylbutanoyl)amino]acetyl)amino)propylphosphonic acid
-
Plasmodium falciparum
3-(hydroxy([(4-phenoxybutanoyl)amino]acetyl)amino)propylphosphonic acid
-
Escherichia coli
3-(hydroxy([(4-phenoxybutanoyl)amino]acetyl)amino)propylphosphonic acid
-
Plasmodium falciparum
3-(hydroxy([(4-phenylbutanoyl)amino]acetyl)amino)propylphosphonic acid
-
Escherichia coli
3-(hydroxy([(4-phenylbutanoyl)amino]acetyl)amino)propylphosphonic acid
-
Plasmodium falciparum
3-([(1H-indol-3-yl)acetyl]amino)propylphosphonic acid
-
Escherichia coli
3-([2-(methoxycarbonyl)benzoyl]amino)propylphosphonic acid
-
Escherichia coli
3-([3-(1H-indol-3-yl)propanoyl]amino)propylphosphonic acid
-
Escherichia coli
3-([4-(1H-indol-3-yl)butanoyl]amino)propylphosphonic acid
-
Escherichia coli
3-[(([(3,4-dimethoxyphenyl)acetyl]amino)acetyl)(hydroxy)amino]propylphosphonic acid
-
Escherichia coli
3-[(([(3,4-dimethoxyphenyl)acetyl]amino)acetyl)(hydroxy)amino]propylphosphonic acid
-
Plasmodium falciparum
3-[(2-hydroxybenzoyl)amino]propylphosphonic acid
-
Escherichia coli
3-[(3,4-diethoxybenzoyl)amino]propylphosphonic acid
-
Escherichia coli
3-[(3,4-dimethoxybenzoyl)amino]propylphosphonic acid
-
Escherichia coli
3-[(4-methylpentanoyl)amino]propylphosphonic acid
-
Escherichia coli
3-[(4-phenoxybenzoyl)amino]propylphosphonic acid
-
Escherichia coli
3-[([(cyclopropylcarbonyl)amino]acetyl)(hydroxy)amino]propylphosphonic acid
-
Escherichia coli
3-[([(cyclopropylcarbonyl)amino]acetyl)(hydroxy)amino]propylphosphonic acid
-
Plasmodium falciparum
3-[hydroxy(([3-(trifluoromethoxy)benzoyl]amino)acetyl)amino]propylphosphonic acid
-
Escherichia coli
3-[hydroxy(([3-(trifluoromethoxy)benzoyl]amino)acetyl)amino]propylphosphonic acid
-
Plasmodium falciparum
3-[hydroxy(([4-(1H-indol-3-yl)butanoyl]amino)acetyl)amino]propylphosphonic acid
-
Escherichia coli
3-[hydroxy(([4-(1H-indol-3-yl)butanoyl]amino)acetyl)amino]propylphosphonic acid
-
Plasmodium falciparum
fosmidomycin
-
Escherichia coli
fosmidomycin
-
Plasmodium falciparum
FR-900098 fosmidomycin homologue Escherichia coli
FR-900098 fosmidomycin homologue Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Plasmodium falciparum
-
-
-

Purification (Commentary)

Purification (Comment) Organism
by immobilized metal affinity chromatography on a Co column, ca. 90% pure Plasmodium falciparum
by immobilized metal affinity chromatography on a Co column, followed by anion exchange chromatography, gel filtration and ultrafiltration Escherichia coli

Storage Stability

Storage Stability Organism
-20°C Escherichia coli
-70°C Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-deoxy-D-xylulose 5-phosphate + NADPH + H+
-
Escherichia coli 2-C-methyl-D-erythritol 4-phosphate + NADP+
-
?
1-deoxy-D-xylulose 5-phosphate + NADPH + H+
-
Plasmodium falciparum 2-C-methyl-D-erythritol 4-phosphate + NADP+
-
?

Synonyms

Synonyms Comment Organism
DXR
-
Escherichia coli
DXR
-
Plasmodium falciparum

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Escherichia coli
NADPH
-
Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000018
-
-
Plasmodium falciparum FR-900098
0.000032
-
-
Plasmodium falciparum fosmidomycin
0.00005
-
-
Escherichia coli fosmidomycin
0.000051
-
-
Escherichia coli FR-900098
0.0004
-
-
Plasmodium falciparum 3-(hydroxy([(4-phenoxybutanoyl)amino]acetyl)amino)propylphosphonic acid
0.001
-
-
Escherichia coli 3-(hydroxy([(4-phenoxybutanoyl)amino]acetyl)amino)propylphosphonic acid
0.0029
-
-
Plasmodium falciparum 3-[hydroxy(([3-(trifluoromethoxy)benzoyl]amino)acetyl)amino]propylphosphonic acid
0.0033
-
-
Plasmodium falciparum 3-[([(cyclopropylcarbonyl)amino]acetyl)(hydroxy)amino]propylphosphonic acid
0.0051
-
-
Escherichia coli 3-[hydroxy(([3-(trifluoromethoxy)benzoyl]amino)acetyl)amino]propylphosphonic acid
0.0066
-
-
Plasmodium falciparum 3-[hydroxy(([4-(1H-indol-3-yl)butanoyl]amino)acetyl)amino]propylphosphonic acid
0.0071
-
-
Escherichia coli 3-[([(cyclopropylcarbonyl)amino]acetyl)(hydroxy)amino]propylphosphonic acid
0.0093
-
-
Plasmodium falciparum 3-(hydroxy([(2-phenylbutanoyl)amino]acetyl)amino)propylphosphonic acid
0.0096
-
-
Plasmodium falciparum 3-(hydroxy([(3-methylbutanoyl)amino]acetyl)amino)propylphosphonic acid
0.012
-
-
Escherichia coli 3-(hydroxy([(3-methylbutanoyl)amino]acetyl)amino)propylphosphonic acid
0.012
-
-
Plasmodium falciparum 3-[(([(3,4-dimethoxyphenyl)acetyl]amino)acetyl)(hydroxy)amino]propylphosphonic acid
0.014
-
-
Escherichia coli 3-[(([(3,4-dimethoxyphenyl)acetyl]amino)acetyl)(hydroxy)amino]propylphosphonic acid
0.017
-
-
Escherichia coli 3-[hydroxy(([4-(1H-indol-3-yl)butanoyl]amino)acetyl)amino]propylphosphonic acid
0.019
-
-
Escherichia coli 3-(hydroxy([(4-phenylbutanoyl)amino]acetyl)amino)propylphosphonic acid
0.02
-
-
Escherichia coli 3-(hydroxy([(2-phenylbutanoyl)amino]acetyl)amino)propylphosphonic acid
0.02
-
-
Plasmodium falciparum 3-(hydroxy([(4-phenylbutanoyl)amino]acetyl)amino)propylphosphonic acid
0.03
-
-
Escherichia coli (3S,4R)-3,4-dihydroxy-4-methyl-5-oxohexylphosphonic acid
0.03
-
-
Escherichia coli 3-([4-(1H-indol-3-yl)butanoyl]amino)propylphosphonic acid
0.03
-
-
Escherichia coli 3-([3-(1H-indol-3-yl)propanoyl]amino)propylphosphonic acid
0.03
-
-
Escherichia coli 3-([(1H-indol-3-yl)acetyl]amino)propylphosphonic acid
0.03
-
-
Escherichia coli 3-([2-(methoxycarbonyl)benzoyl]amino)propylphosphonic acid
0.03
-
-
Escherichia coli 3-[(2-hydroxybenzoyl)amino]propylphosphonic acid
0.03
-
-
Escherichia coli 3-[(3,4-diethoxybenzoyl)amino]propylphosphonic acid
0.03
-
-
Escherichia coli 3-[(4-methylpentanoyl)amino]propylphosphonic acid
0.03
-
-
Escherichia coli 3-[(4-phenoxybenzoyl)amino]propylphosphonic acid
0.03
-
-
Escherichia coli 3-[(3,4-dimethoxybenzoyl)amino]propylphosphonic acid