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Literature summary extracted from

  • Vanichtanankul, J.; Taweechai, S.; Yuvaniyama, J.; Vilaivan, T.; Chitnumsub, P.; Kamchonwongpaisan, S.; Yuthavong, Y.
    Trypanosomal dihydrofolate reductase reveals natural antifolate resistance (2011), ACS Chem. Biol., 6, 905-911.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.5.1.3 expressed in Escherichia coli BL21(DE3) cells Trypanosoma brucei

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.5.1.3 in complex with NADPH and inhibitors, hanging drop vapor diffusion method, using Trypanosoma brucei

Protein Variants

EC Number Protein Variants Comment Organism
1.5.1.3 T86N the mutant shows reduced catalytic efficiency compared to the wild type enzyme Trypanosoma brucei
1.5.1.3 T86S the mutant shows reduced catalytic efficiency compared to the wild type enzyme Trypanosoma brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 cycloguanil
-
 Trypanosoma brucei
1.5.1.3 pyrimethamine
-
 Trypanosoma brucei
1.5.1.3 WR99210
-
 Trypanosoma brucei

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.5.1.3 0.00385
-
 7,8-dihydrofolate wild type enzyme, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.00443
-
 NADPH wild type enzyme, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.00523
-
 NADPH mutant enzyme T86N, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.00792
-
 NADPH mutant enzyme T86S, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.01625
-
 7,8-dihydrofolate mutant enzyme T86S, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.03051
-
 7,8-dihydrofolate mutant enzyme T86N, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.5.1.3 7,8-dihydrofolate + NADPH + H+ Trypanosoma brucei
-
 5,6,7,8-tetrahydrofolate + NADP+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Trypanosoma brucei
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.5.1.3 methotrexate-Sepharose column chromatography, SP-Sepharose column chromatography, and Sephacryl S-200 and gel filtration Trypanosoma brucei

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
1.5.1.3 DHFR
-
 Trypanosoma brucei

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.5.1.3 3.11
-
 7,8-dihydrofolate wild type enzyme, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 3.75
-
 7,8-dihydrofolate mutant enzyme T86N, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 4.54
-
 7,8-dihydrofolate mutant enzyme T86S, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei

Cofactor

EC Number Cofactor Comment Organism Structure
1.5.1.3 NADPH
-
 Trypanosoma brucei

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.5.1.3 0.0000009
-
 WR99210 mutant enzyme T86S, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.0000011
-
 WR99210 wild type enzyme, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.0000021
-
 pyrimethamine mutant enzyme T86S, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.0000039
-
 WR99210 mutant enzyme T86N, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.0000205
-
 cycloguanil mutant enzyme T86S, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.000024
-
 pyrimethamine wild type enzyme, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.000179
-
 pyrimethamine mutant enzyme T86N, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.000256
-
 cycloguanil wild type enzyme, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 0.001915
-
 cycloguanil mutant enzyme T86N, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1.5.1.3 120
-
 7,8-dihydrofolate mutant enzyme T86N, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 280
-
 7,8-dihydrofolate mutant enzyme T86S, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei
1.5.1.3 810
-
 7,8-dihydrofolate wild type enzyme, in 50 mM TES, pH 7.0, at 37°C Trypanosoma brucei