Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Perez-Abraham, R.; Sanchez, K.; Alfonso, M.; Gubler, U.; Siekierka, J.; Goodey, N.
    Expression, purification and enzymatic characterization of Brugia malayi dihydrofolate reductase (2016), Protein Expr. Purif., 128, 81-85 .
    View publication on PubMed

Application

EC Number Application Comment Organism
1.5.1.3 drug development dihydrofolate reductase is a potential drug target for the elimination of Brugia malayi, one of the three causative agents of lymphatic filariasis, a parasitic disease Brugia malayi

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.5.1.3 sequence comparisons, recombinant expression of His6-tagged enzyme in Escherichia coli strain BL21(DE3) Brugia malayi

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 2,4-diaminopyrimidine poor inhibition Brugia malayi
1.5.1.3 2,4-diaminoquinazoline low inhibition Brugia malayi
1.5.1.3 cycloguanil low inhibition Brugia malayi
1.5.1.3 methotrexate strong inhibition Brugia malayi
1.5.1.3 additional information antifolate compounds can serve as inhibitors of BmDHFR Brugia malayi
1.5.1.3 pyrimethamine
-
 Brugia malayi
1.5.1.3 trimethoprim
-
 Brugia malayi

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.5.1.3 additional information
-
 additional information Michaelis-Menten steady-state kinetics Brugia malayi
1.5.1.3 0.0147
-
 7,8-dihydrofolate above, pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi

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+ Brugia malayi
-
 5,6,7,8-tetrahydrofolate + NADP+
-
 r

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Brugia malayi
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.5.1.3 recombinant His6-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography Brugia malayi

Substrates and Products (Substrate)

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

Subunits

EC Number Subunits Comment Organism
1.5.1.3 ? x * 22000, recombinant His6-tagged enzyme, SDS-PAGE, x * 22086, sequence calculation, His-tagged enzyme Brugia malayi

Synonyms

EC Number Synonyms Comment Organism
1.5.1.3 BmDHFR
-
 Brugia malayi
1.5.1.3 DHFR
-
 Brugia malayi

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.5.1.3 25
-
 assay at Brugia malayi

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.5.1.3 1.4
-
 7,8-dihydrofolate above, pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.5.1.3 6
-
 assay at Brugia malayi

Cofactor

EC Number Cofactor Comment Organism Structure
1.5.1.3 NADP+
-
 Brugia malayi
1.5.1.3 NADPH the equilibrium dissociation constant KD for NADPH is 25nM Brugia malayi

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.5.1.3 additional information
-
 additional information inhibition kinetics Brugia malayi
1.5.1.3 0.0000013
-
 methotrexate pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi
1.5.1.3 0.013
-
 pyrimethamine pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi
1.5.1.3 0.046
-
 trimethoprim pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi
1.5.1.3 0.065
-
 2,4-diaminopyrimidine pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi
1.5.1.3 0.459
-
 2,4-diaminoquinazoline pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi
1.5.1.3 8
-
 cycloguanil above, pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.5.1.3 0.0000031
-
 pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi methotrexate
1.5.1.3 0.032
-
 pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi trimethoprim
1.5.1.3 0.109
-
 pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi pyrimethamine
1.5.1.3 0.154
-
 pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi 2,4-diaminoquinazoline
1.5.1.3 0.771
-
 pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi cycloguanil
1.5.1.3 20
-
 above, pH 6.0, 25°C recombinant His-tagged enzyme Brugia malayi 2,4-diaminopyrimidine

General Information

EC Number General Information Comment Organism
1.5.1.3 additional information the predicted specificity determining positions in BmDHFR for ligand binding are Val5, Gly12, Met27, Asn44, Ala45, Lys51, Phe60, Val84, Phe89 Leu95, Leu96, Gly133, Ala137, Val139, Phe140, Phe141 and Glu169 Brugia malayi