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Literature summary extracted from

  • Pornthanakasem, W.; Riangrungroj, P.; Chitnumsub, P.; Ittarat, W.; Kongkasuriyachai, D.; Uthaipibull, C.; Yuthavong, Y.; Leartsakulpanich, U.
    Role of Plasmodium vivax dihydropteroate synthase polymorphisms in sulfa drug resistance (2016), Antimicrob. Agents Chemother., 60, 4453-4463 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.5.1.15 expression in Escherichia coli Rosetta(DE3)pLysS Plasmodium vivax

Protein Variants

EC Number Protein Variants Comment Organism
2.5.1.15 A383G mutation does not much influence the enzyme catalytic activity. Mutant becomes 13fold more resistant to sulfadoxine than the wild type Plasmodium vivax
2.5.1.15 A383G/A553G mutation does not much influence the enzyme catalytic activity. Mutant becomes 13fold more resistant to sulfadoxine than the wild type Plasmodium vivax
2.5.1.15 S382A/A383G/A553G mutation does not much influence the enzyme catalytic activity. Mutant becomes 13fold more resistant to sulfadoxine than the wild type Plasmodium vivax
2.5.1.15 V585A 2fold increase in the level of resistance to sulfadoxine compared with that of the wild type carrying V585A. V585A mutant is 4fold more resistant to dapsone than the wild type Plasmodium vivax

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.15 dapsone
-
 Plasmodium vivax
2.5.1.15 sulfadoxine
-
 Plasmodium vivax
2.5.1.15 sulfathiazole
-
 Plasmodium vivax

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.5.1.15 0.00015
-
 4-Aminobenzoate wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.00019
-
 4-Aminobenzoate mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.00026
-
 4-Aminobenzoate mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.00033
-
 4-Aminobenzoate mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.00048
-
 4-Aminobenzoate mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.5.1.15 174000
-
 gel filtration Plasmodium vivax

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.5.1.15 (7,8-dihydropterin-6-yl)methyl diphosphate + 4-aminobenzoate Plasmodium vivax
-
 diphosphate + 7,8-dihydropteroate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.15 Plasmodium vivax
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.5.1.15
-
 Plasmodium vivax

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.15 (7,8-dihydropterin-6-yl)methyl diphosphate + 4-aminobenzoate
-
 Plasmodium vivax diphosphate + 7,8-dihydropteroate
-
 ?

Subunits

EC Number Subunits Comment Organism
2.5.1.15 homodimer 2 * 85000, SDS-PAGE Plasmodium vivax

Synonyms

EC Number Synonyms Comment Organism
2.5.1.15 DHPS-HPPK bifunctional enzyme Plasmodium vivax
2.5.1.15 dihydropteroate synthase/hydroxymethyldihydropterin pyrophosphokinase bifunctional enzyme Plasmodium vivax

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.5.1.15 0.0024
-
 4-Aminobenzoate wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.0024
-
 (7,8-dihydropterin-6-yl)methyl diphosphate wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.0029
-
 4-Aminobenzoate mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.0029
-
 (7,8-dihydropterin-6-yl)methyl diphosphate mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.0055
-
 4-Aminobenzoate mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.0055
-
 (7,8-dihydropterin-6-yl)methyl diphosphate mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.006
-
 4-Aminobenzoate mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.006
-
 (7,8-dihydropterin-6-yl)methyl diphosphate mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.0134
-
 4-Aminobenzoate mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.0134
-
 (7,8-dihydropterin-6-yl)methyl diphosphate mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.5.1.15 0.00011
-
 dapsone wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.00015
-
 sulfathiazole wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.00019
-
 sulfathiazole mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.00053
-
 dapsone mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.0015
-
 sulfadoxine wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.00295
-
 sulfathiazole mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.003
-
 sulfadoxine mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.00367
-
 dapsone mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.00454
-
 dapsone mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.01553
-
 sulfathiazole mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.01773
-
 dapsone mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.019
-
 sulfathiazole mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.0481
-
 sulfadoxine mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.176
-
 sulfadoxine mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax
2.5.1.15 0.227
-
 sulfadoxine mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax

General Information

EC Number General Information Comment Organism
2.5.1.15 drug target the enzyme is a sulfa drug target in malaria treatment Plasmodium vivax