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Literature summary for 1.5.1.3 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

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

Inhibitors

Inhibitors Comment Organism Structure
cycloguanil
-
Plasmodium falciparum
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
pyrimethamine
-
Plasmodium falciparum
WR99210
-
Plasmodium falciparum

KM Value [mM]

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

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Specific Activity [micromol/min/mg]

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

Substrates and Products (Substrate)

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

Turnover Number [1/s]

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

pH Range

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

Ki Value [mM]

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