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Literature summary extracted from

  • Kamchonwongpaisan, S.; Vanichtanankul, J.; Taweechai, S.; Chitnumsub, P.; Yuthavong, Y.
    The role of tryptophan-48 in catalysis and binding of inhibitors of Plasmodium falciparum dihydrofolate reductase (2007), Int. J. Parasitol., 37, 787-793.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
1.5.1.3 additional information construction of 19 mutants of residue W48. All mutants show very low specific activites Plasmodium falciparum
1.5.1.3 W48Y 3% of wild-type activity Plasmodium falciparum
1.5.1.3 W48Y/N188Y 28.9% of wild-type activity Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 cycloguanil
-
 Plasmodium falciparum
1.5.1.3 additional information in presence of up to 4 M urea, wild-type retains more than 80% of its catalytic activity. Mutant W48Y loses more than 20% of activity in presence of 1 M urea Plasmodium falciparum
1.5.1.3 pyrimethamine
-
 Plasmodium falciparum
1.5.1.3 WR99210
-
 Plasmodium falciparum

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.5.1.3 0.0027
-
 NADPH wild-type, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.00345
-
 NADPH mutant W48Y/N188Y, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.0045
-
 NADPH mutant W48Y, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.0051
-
 7,8-dihydrofolate wild-type, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.0231
-
 7,8-dihydrofolate mutant W48Y, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.0324
-
 7,8-dihydrofolate mutant W48Y/N188Y, 25°C, pH 7.0 Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Plasmodium falciparum
-
-
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.5.1.3 0.82
-
 wild-type, 25°C, pH 7.0 Plasmodium falciparum

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.5.1.3 7,8-dihydrofolate + NADPH + H+
-
 Plasmodium falciparum 5,6,7,8-tetrahydrofolate + NADP+
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.5.1.3 2.8
-
 NADPH mutant W48Y, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 3.3
-
 NADPH mutant W48Y/N188Y, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 60.9
-
 NADPH wild-type, 25°C, pH 7.0 Plasmodium falciparum

pH Range

EC Number pH Minimum pH Maximum Comment Organism
1.5.1.3 4 6.5 mutant W48Y, more than 60% of maximum activity Plasmodium falciparum
1.5.1.3 4 7.5 wild-type, more than 60% of maximum activity Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.5.1.3 0.00000044
-
 WR99210 wild-type, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.00000072
-
 pyrimethamine wild-type, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.000001
-
 pyrimethamine mutant W48Y/N188Y, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.000001
-
 cycloguanil wild-type, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.00000121
-
 WR99210 mutant W48Y/N188Y, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.00000154
-
 WR99210 mutant W48Y, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.00000174
-
 pyrimethamine mutant W48Y, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.00000199
-
 cycloguanil mutant W48Y/N188Y, 25°C, pH 7.0 Plasmodium falciparum
1.5.1.3 0.00000548
-
 cycloguanil mutant W48Y, 25°C, pH 7.0 Plasmodium falciparum