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Literature summary extracted from

  • Sirawaraporn, W.; Yongkiettrakul, S.; Sirawaraporn, R.; Yuthavong, Y.; Santi, D.V.
    Plasmodium falciparum: asparagine mutant at residue 108 of dihydrofolate reductase is an optimal antifolate-resistant single mutant (1997), Exp. Parasitol., 87, 245-252.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.5.1.3 expression of wild-type and mutant enzymes in Escherichia coli Plasmodium falciparum

Protein Variants

EC Number Protein Variants Comment Organism
1.5.1.3 S108A combinatorial mutagenesis Plasmodium falciparum
1.5.1.3 S108C combinatorial mutagenesis Plasmodium falciparum
1.5.1.3 S108D combinatorial mutagenesis, no detectable activity on refolding from inclusion bodies Plasmodium falciparum
1.5.1.3 S108E combinatorial mutagenesis, no detectable activity on refolding from inclusion bodies Plasmodium falciparum
1.5.1.3 S108F combinatorial mutagenesis, no detectable activity on refolding from inclusion bodies Plasmodium falciparum
1.5.1.3 S108G combinatorial mutagenesis Plasmodium falciparum
1.5.1.3 S108H combinatorial mutagenesis, no detectable activity on refolding from inclusion bodies Plasmodium falciparum
1.5.1.3 S108I combinatorial mutagenesis, no detectable activity on refolding from inclusion bodies Plasmodium falciparum
1.5.1.3 S108L combinatorial mutagenesis, reduced activity Plasmodium falciparum
1.5.1.3 S108M combinatorial mutagenesis, reduced activity Plasmodium falciparum
1.5.1.3 S108N combinatorial mutagenesis, conferred resistance to pyrimethamine and cycloguanil Plasmodium falciparum
1.5.1.3 S108P combinatorial mutagenesis, no detectable activity on refolding from inclusion bodies Plasmodium falciparum
1.5.1.3 S108Q combinatorial mutagenesis, reduced activity, conferred resistance to pyrimethamine and cycloguanil Plasmodium falciparum
1.5.1.3 S108R combinatorial mutagenesis, no detectable activity on refolding from inclusion bodies Plasmodium falciparum
1.5.1.3 S108T combinatorial mutagenesis, reduced activity Plasmodium falciparum
1.5.1.3 S108V combinatorial mutagenesis, reduced activity Plasmodium falciparum
1.5.1.3 S108W combinatorial mutagenesis, no detectable activity on refolding from inclusion bodies Plasmodium falciparum
1.5.1.3 S108Y combinatorial mutagenesis, no detectable activity on refolding from inclusion bodies Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 cycloguanil wild-type and several Ser108 mutant enzymes Plasmodium falciparum
1.5.1.3 pyrimethamine wild-type and several mutants of Ser108 Plasmodium falciparum

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.5.1.3 0.005
-
 NADPH recombinant wild-type enzyme Plasmodium falciparum
1.5.1.3 0.007
-
 NADPH recombinant mutant S108N Plasmodium falciparum
1.5.1.3 0.009
-
 NADPH recombinant mutants S108G, S108A and S108C Plasmodium falciparum
1.5.1.3 0.013
-
 7,8-dihydrofolate recombinant wild-type enzyme Plasmodium falciparum
1.5.1.3 0.014
-
 7,8-dihydrofolate recombinant mutants S108T and S108A Plasmodium falciparum
1.5.1.3 0.014
-
 NADPH recombinant mutant S108Q Plasmodium falciparum
1.5.1.3 0.017
-
 NADPH recombinant mutant S108T Plasmodium falciparum
1.5.1.3 0.02 0.025 7,8-dihydrofolate recombinant mutants S108G, S108N and S108C Plasmodium falciparum
1.5.1.3 0.05
-
 7,8-dihydrofolate recombinant mutant S108Q Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Plasmodium falciparum
-
 several Ser108 mutants
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.5.1.3 refolding and purification of wild-type and mutant enzymes from inclusion bodies in Escherichia coli Plasmodium falciparum

Renatured (Commentary)

EC Number Renatured (Comment) Organism
1.5.1.3 refolding of recombinant enzymes from inclusion bodies due to expression in E. coli 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 0.6 0.7 recombinant mutants S108V and S108M Plasmodium falciparum
1.5.1.3 1
-
 recombinant mutants S108C and S108L Plasmodium falciparum
1.5.1.3 2
-
 recombinant mutant S108A Plasmodium falciparum
1.5.1.3 4
-
 recombinant mutant S108G Plasmodium falciparum
1.5.1.3 5
-
 recombinant mutant S108Q Plasmodium falciparum
1.5.1.3 8
-
 recombinant mutant S108T Plasmodium falciparum
1.5.1.3 9
-
 recombinant mutant S108N Plasmodium falciparum
1.5.1.3 17
-
 recombinant wild-type enzyme Plasmodium falciparum

Storage Stability

EC Number Storage Stability Organism
1.5.1.3 -20°C, 20 mM potassium phosphate, pH 7.0, 0.1 mM EDTA, 10 mM dithiothreitol, 0.2 M KCl, 20% glycerol, mutant S108Q loss of 40% activity after 7 months Plasmodium falciparum
1.5.1.3 -20°C, 20 mM potassium phosphate, pH7.0, 0.1 mM EDTA, 10 mM dithiothreitol, 0.2 M KCl, 20% glycerol, mutants S108G, S108A and S108C stable over 7 months Plasmodium falciparum

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.5.1.3 12
-
 7,8-dihydrofolate recombinant mutant S108C Plasmodium falciparum
1.5.1.3 21
-
 7,8-dihydrofolate recombinant mutant S108A Plasmodium falciparum
1.5.1.3 23
-
 7,8-dihydrofolate recombinant mutant S108G Plasmodium falciparum
1.5.1.3 36
-
 7,8-dihydrofolate recombinant mutant S108T Plasmodium falciparum
1.5.1.3 37
-
 7,8-dihydrofolate recombinant mutant S108Q Plasmodium falciparum
1.5.1.3 88
-
 7,8-dihydrofolate recombinant wild-type enzyme Plasmodium falciparum
1.5.1.3 92
-
 7,8-dihydrofolate recombinant mutant S108N Plasmodium falciparum

Cofactor

EC Number Cofactor Comment Organism Structure
1.5.1.3 NADPH
-
 Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.5.1.3 0.0000014
-
 pyrimethamine recombinant mutant S108T Plasmodium falciparum
1.5.1.3 0.0000015
-
 pyrimethamine recombinant wild-type enzyme Plasmodium falciparum
1.5.1.3 0.0000016
-
 cycloguanil recombinant mutant S108T Plasmodium falciparum
1.5.1.3 0.000002
-
 cycloguanil recombinant mutant S108A Plasmodium falciparum
1.5.1.3 0.0000026
-
 cycloguanil recombinant wild-type enzyme Plasmodium falciparum
1.5.1.3 0.000003
-
 cycloguanil recombinant mutant S108C Plasmodium falciparum
1.5.1.3 0.000004
-
 pyrimethamine recombinant mutant S108A Plasmodium falciparum
1.5.1.3 0.000006
-
 pyrimethamine recombinant mutant S108C Plasmodium falciparum
1.5.1.3 0.000007
-
 pyrimethamine recombinant mutant S108G Plasmodium falciparum
1.5.1.3 0.000013
-
 pyrimethamine recombinant mutant S108N Plasmodium falciparum
1.5.1.3 0.000015
-
 cycloguanil recombinant mutant S108N Plasmodium falciparum
1.5.1.3 0.000017
-
 cycloguanil recombinant mutant S108G Plasmodium falciparum
1.5.1.3 0.000095
-
 pyrimethamine recombinant mutant S108Q Plasmodium falciparum
1.5.1.3 0.000158
-
 cycloguanil recombinant mutant S108Q Plasmodium falciparum